TAMATINIB

Details

Stereochemistry	ACHIRAL
Molecular Formula	C22H23FN6O5
Molecular Weight	470.4536
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

COC1=CC(NC2=NC=C(F)C(NC3=CC=C4OC(C)(C)C(=O)NC4=N3)=N2)=CC(OC)=C1OC

InChI

InChIKey=NHHQJBCNYHBUSI-UHFFFAOYSA-N

InChI=1S/C22H23FN6O5/c1-22(2)20(30)28-19-13(34-22)6-7-16(27-19)26-18-12(23)10-24-21(29-18)25-11-8-14(31-3)17(33-5)15(9-11)32-4/h6-10H,1-5H3,(H3,24,25,26,27,28,29,30)

HIDE SMILES / InChI

Molecular Formula	C22H23FN6O5
Molecular Weight	470.4536
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/16946104 | http://adisinsight.springer.com/drugs/800021937

R406 (TAMATINIB) is an ATP-competitive inhibitor of spleen tyrosine kinase (Syk), which plays a key role in the signaling of activating Fc receptors and the B-cell receptor (BCR). R406 blocked Syk-dependent FcR-mediated activation of monocytes/macrophages and neutrophils and BCR-mediated activation of B lymphocytes. R406 was selective as assessed using a large panel of Syk-independent cell-based assays representing both specific and general signaling pathways. Consistent with Syk inhibition, oral administration of R406 to mice reduced immune complex-mediated inflammation in a reverse-passive Arthus reaction and two antibody-induced arthritis models. R406 is the active compound of pro-drug Fostamatinib (R-788). Fostamatinib is being developed by Rigel Pharmaceuticals for the treatment of immune thrombocytopenic purpura (ITP) and IgA nephropathy.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Tyrosine-protein kinase SYK 22 Target ID: CHEMBL2599 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16946104	Inhibitor 8504		30.0 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Immune thrombocytopenia 10 Sources: http://adisinsight.springer.com/drugs/800021937	Primary		Phase III 665	Unknown Approved Use Unknown
IgA nephropathy 4 Sources: http://adisinsight.springer.com/drugs/800021937	Primary		Phase II 1147	Unknown Approved Use Unknown

C_max

Value	Dose	Analyte	Population
501 ng/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2030 ng/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	250 mg single, oral dose: 250 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3410 ng/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3660 ng/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3920 ng/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
306 ng/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
1140 ng/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	250 mg single, oral dose: 250 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
1220 ng/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
682 ng/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
605 ng/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	75 mg single, oral dose: 75 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
363 ng/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	75 mg single, oral dose: 75 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
747 ng/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	160 mg 2 times / day multiple, oral dose: 160 mg route of administration: Oral experiment type: MULTIPLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
1530 ng/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	160 mg 2 times / day steady-state, oral dose: 160 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
397 ng/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	100 mg 2 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	R406 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
761 ng/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	100 mg 2 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	R406 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
690 ng/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
425 ng/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
407 ng/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
529 ng/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
692 ng/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
615 ng/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
602 ng/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
582 ng/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED

AUC

Value	Dose	Analyte	Population
4410 ng × h/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
18100 ng × h/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	250 mg single, oral dose: 250 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
34900 ng × h/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
29600 ng × h/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
36600 ng × h/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3150 ng × h/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
13700 ng × h/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	250 mg single, oral dose: 250 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
13400 ng × h/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
7510 ng × h/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
6490 ng × h/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	75 mg single, oral dose: 75 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
7140 ng × h/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	75 mg single, oral dose: 75 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
8250 ng × h/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	160 mg 2 times / day multiple, oral dose: 160 mg route of administration: Oral experiment type: MULTIPLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
19900 ng × h/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	160 mg 2 times / day steady-state, oral dose: 160 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
3260 ng × h/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	100 mg 2 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	R406 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
6750 ng × h/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
6110 ng × h/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
4950 ng × h/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
6280 ng × h/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
8970 ng × h/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
6390 ng × h/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
6860 ng × h/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
9490 ng × h/mL REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED

T_1/2

Value	Dose	Analyte	Population
14.5 h REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
14.9 h REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	250 mg single, oral dose: 250 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
17.8 h REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
20.9 h REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
12.9 h REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
14.8 h REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
16 h REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	250 mg single, oral dose: 250 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
12.1 h REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
19 h REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
17.9 h REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	75 mg single, oral dose: 75 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
18.4 h REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	75 mg single, oral dose: 75 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
19.9 h REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	160 mg 2 times / day multiple, oral dose: 160 mg route of administration: Oral experiment type: MULTIPLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
14.5 h REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	100 mg 2 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	R406 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
20.4 h REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	100 mg 2 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	R406 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
20.5 h REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
23.8 h REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
19.6 h REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
22.1 h REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
19.4 h REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
16.7 h REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
16.1 h REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
19.2 h REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	R406 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED

F_unbound

Value	Dose	Co-administered	Analyte	Population
3.7% REVIEW https://link.springer.com/article/10.1007/s40262-022-01135-0	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:		R406 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	DY110886	https://www.001chemical.com/chem/search?q=DY110886
1PlusChem LLC	1P008HDZ	https://www.1pchem.com/search?query=1P008HDZ
1PlusChem LLC	1P00G46D	https://www.1pchem.com/search?query=1P00G46D
AChemBlock	A-624	http://www.achemblock.com/catalogsearch/result/?q=A-624
AK Scientific	SYN1121	https://aksci.com/item_detail.php?cat=SYN1121
AK Scientific	X7372	https://aksci.com/item_detail.php?cat=X7372
AK Scientific	X7500	https://aksci.com/item_detail.php?cat=X7500
Ambeed	A104426	http://www.ambeed.com/search/Search.html?keyword=A104426
Ambeed	A233735	http://www.ambeed.com/search/Search.html?keyword=A233735
Angene	AGN-PC-00J96O	http://www.angenechemical.com/productshow/AGN-PC-00J96O.html
AOBIOUS INC	AOB87473	http://aobious.com/aobious/search?search_query=AOB87473
ApexBio Technology	A5880	https://www.apexbt.com/catalogsearch/result/?q=A5880
ApexBio Technology	A8546	https://www.apexbt.com/catalogsearch/result/?q=A8546
AstaTech	41362	http://astatechinc.com/CPSResult.php?CRNO=41362
AstaTech	41577	http://astatechinc.com/CPSResult.php?CRNO=41577
Axon MedChem	1674	https://www.axonmedchem.com/product/1674
BLD Pharm	BD208780	http://www.bldpharm.com/search/Search.html?keyword=BD208780
BLD Pharm	BD448256	http://www.bldpharm.com/search/Search.html?keyword=BD448256
BOC Sciences	841290-80-0	http://www.bocsci.com/description.asp?cas=841290-80-0
Capot Chemical	22483	https://www.capotchem.com/search.do?q=22483
Cayman Chemical	11422	http://www.caymanchem.com/app/template/Product.vm/catalog/11422
Chem Scene	CS-0229	http://www.chemscene.com/goproductList/searchProductList?productObj=CS-0229
Chem Scene	CS-0436	http://www.chemscene.com/goproductList/searchProductList?productObj=CS-0436
ChemShuttle	101146	https://www.chemshuttle.com/catalogsearch/result/?q=101146
ChemShuttle	111912	https://www.chemshuttle.com/catalogsearch/result/?q=111912
Combi-Blocks	QV-8534	http://www.combi-blocks.com/cgi-bin/find.cgi?QV-8534
Combi-Blocks	QW-3656	http://www.combi-blocks.com/cgi-bin/find.cgi?QW-3656
eMolecules	275062895	https://orderbb.emolecules.com/search/#?query=275062895
eMolecules	31592812	https://orderbb.emolecules.com/search/#?query=31592812
eMolecules	32278236	https://orderbb.emolecules.com/search/#?query=32278236
eNovation Chemicals	D372375	https://www.enovationchem.com/Products.asp?SEARCHTEXT=D372375&searchbtn.x=0&searchbtn.y=0
eNovation Chemicals	D372376	https://www.enovationchem.com/Products.asp?SEARCHTEXT=D372376&searchbtn.x=0&searchbtn.y=0
Excenen	EX-A103	http://www.excenen.com/searchresultlist.php?id=EX-A103-1
Excenen	EX-A103-1	http://www.excenen.com/searchresultlist.php?id=EX-A103-1
Hairui	HR107242	http://www.hairuichem.com/en/product/search.do?q=HR107242
KeyOrganics	AS-16262	http://www.keyorganicsinc.com/bionet/catalogsearch/result?q=AS-16262
KeyOrganics	AS-55802	http://www.keyorganicsinc.com/bionet/catalogsearch/result?q=AS-55802
Lab Seeker	SC-84778	http://www.labseeker.com/search.php?keywords=SC-84778&category=0
Lab Seeker	SC-85833	http://www.labseeker.com/search.php?keywords=SC-85833&category=0
LabSeeker	SC-84778	http://www.labseeker.com/search.php?keywords=SC-84778&category=0
LabSeeker	SC-85833	http://www.labseeker.com/search.php?keywords=SC-85833&category=0
Matrix Scientific	143803	http://www.matrixscientific.com/143803.html
Matrix Scientific	147248	http://www.matrixscientific.com/147248.html
mcule	MCULE-2828803347	https://mcule.com/MCULE-2828803347/
mcule	MCULE-4054807175	https://mcule.com/MCULE-4054807175/
MedChem Express	HY-11108	https://www.medchemexpress.com/search.html?q=HY-11108&ft=&fa=&fp=
MedChem Express	HY-12067	https://www.medchemexpress.com/search.html?q=HY-12067&ft=&fa=&fp=
Molcore	MC110886	http://www.molcore.com/CatMC110886.html
Molnova	M16126	https://www.molnova.com/en/serch-list.html?keywords=M16126
Molnova	M16127	https://www.molnova.com/en/serch-list.html?keywords=M16127
MolPort	MolPort-009-679-442	https://www.molport.com/shop/molecule-link/MolPort-009-679-442
MolPort	MolPort-016-633-305	https://www.molport.com/shop/molecule-link/MolPort-016-633-305
MuseChem	I005038	https://www.musechem.com/product/I005038.html
MuseChem	I008958	https://www.musechem.com/product/I008958.html
Ryan Scientific	TG6-10-1	https://ryansci.com/products?q=TG6-10-1&list_q=&search_type=exact
Selleck Chemicals	S2194	http://www.selleckchem.com/search.html?searchDTO.searchParam=S2194
ShangHai Biochempartner	BCP000195	http://www.biochempartner.com/search_BCP000195
ShangHai Biochempartner	BCP001644	http://www.biochempartner.com/search_BCP001644
ShangHai Biochempartner	BCP01933	http://www.biochempartner.com/search_BCP01933
ShangHai Biochempartner	BCP14809	http://www.biochempartner.com/search_BCP14809
TargetMol	T2467	https://www.targetmol.com/search?keyword=T2467
TargetMol	T6174	https://www.targetmol.com/search?keyword=T6174
Tetrahedron	TS86284	http://www.thsci.com/search.do?q=TS86284
Toronto Research Chemicals	E917527	https://www.trc-canada.com/product-detail/?CatNum=E917527
Toronto Research Chemicals	F596600	https://www.trc-canada.com/product-detail/?CatNum=F596600
Toronto Research Chemicals	G625102	https://www.trc-canada.com/product-detail/?CatNum=G625102
Toronto Research Chemicals	R060000	https://www.trc-canada.com/product-detail/?CatNum=R060000

PubMed

Title	Date	PubMed
R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation.	2006 Dec	16946104
The Syk-kinase inhibitor R406 impairs platelet activation and monocyte tissue factor expression triggered by heparin-PF4 complex directed antibodies.	2011 Oct	21848694

Patents

Sample Use Guides

In Vivo Use Guide

Pharmacokinetic assessment indicated that R406 was highly bioavailable. R406 plasma concentration increased in a dose-proportional fashion up to 400 mg and then reached a plateau. The maximal R406 concentration was generally reached between 1.2 and 1.3 h after dosing, and the half-life was approximately 15 h.

Route of Administration: Oral

In Vitro Use Guide

BCR triggering increases CLL cell viability, and 5 uM R406 abrogates BCR-derived survival signals

Substance Class	Chemical Created by `admin` on `Mon Mar 31 23:32:51 GMT 2025` Edited by `admin` on `Mon Mar 31 23:32:51 GMT 2025`
Record UNII	RC3A285J2G
Record Status	`Validated (UNII)`
Record Version