GALUNISERTIB

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C22H19N5O
Molecular Weight	369.4192
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

CC1=CC=CC(=N1)C2=NN3CCCC3=C2C4=C5C=C(C=CC5=NC=C4)C(N)=O

InChI

InChIKey=IVRXNBXKWIJUQB-UHFFFAOYSA-N

InChI=1S/C22H19N5O/c1-13-4-2-5-18(25-13)21-20(19-6-3-11-27(19)26-21)15-9-10-24-17-8-7-14(22(23)28)12-16(15)17/h2,4-5,7-10,12H,3,6,11H2,1H3,(H2,23,28)

HIDE SMILES / InChI

Molecular Formula	C22H19N5O
Molecular Weight	369.4192
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

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

Description

Galunisertib is a potent inhibitor of TGF beta type 1 receptor. The drug is under clinical development for the treatment of different cancers: pancreatic, hepatocellular, breast, rectal, prostate etc. and reached phase 2/3 in patients with myelodysplastic syndromes.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
TGF-beta receptor type I 6	Inhibitor 8,297		56.0 nM [IC50]

Conditions

Condition	Modality	Highest Phase	Product
Myelodysplastic syndromes 58	Primary	Phase III 656	Unknown
Prostate cancer 178	Primary	Phase II 1,132	Unknown
Rectal adenocarcinoma 2	Primary	Phase II 1,132	Unknown
Hepatocellular carcinoma 83	Primary	Phase II 1,132	Unknown
Breast cancer 434	Primary	Phase II 1,132	Unknown
Pancreatic ductal adenocarcinoma 14	Primary	Phase II 1,132	Unknown
Glioblastoma 65	Primary	Phase II 1,132	Unknown

Sourcing

Sourcing

Show entries

Vendor/Aggregator	ID	URL
001 Chemical	DY116175	https://www.001chemical.com/chem/search?q=DY116175
1PlusChem LLC	1P003497	https://www.1pchem.com/search?query=1P003497
A2B Chem	AB44683	http://a2bchem.com/prod/AB44683
AA Blocks	AA0033PR	http://aablocks.com/goods/Goods/detail?id=AA0033PR
AChemBlock	10348	http://www.achemblock.com/catalogsearch/result/?q=10348

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PubMed

Show entries

Title	Date	PubMed
		252160190
TGFβR1 Blockade with Galunisertib (LY2157299) Enhances Anti-Neuroblastoma Activity of the Anti-GD2 Antibody Dinutuximab (ch14.18) with Natural Killer Cells.	2017 Feb 1	27756784

Showing 1 to 2 of 2 entries

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Patents

Sample Use Guides

In Vivo Use Guide

Patients receive 150 milligrams of galunisertib, given orally twice daily for 14 days followed by 14 days with no study drug (28 day cycles).

Route of Administration: Oral

In Vitro Use Guide

JHH6, SK-HEP1, SK-Sora, HepG2, Hep3B, and HuH7 cells were simultaneously exposed to 0.1, 1, 10, and 100 uM galunisertib with 5 uM sorafenib in presence of TGF-beta for 72 hours.