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Details

Stereochemistry ABSOLUTE
Molecular Formula C19H23N7O2.C3H6O3
Molecular Weight 471.5096
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of AT-9283 L-LACTATE

SMILES

C[C@H](O)C(O)=O.O=C(NC1CC1)NC2=CNN=C2C3=NC4=C(N3)C=CC(CN5CCOCC5)=C4

InChI

InChIKey=RWYNKTMXFIMBFE-WNQIDUERSA-N
InChI=1S/C19H23N7O2.C3H6O3/c27-19(21-13-2-3-13)24-16-10-20-25-17(16)18-22-14-4-1-12(9-15(14)23-18)11-26-5-7-28-8-6-26;1-2(4)3(5)6/h1,4,9-10,13H,2-3,5-8,11H2,(H,20,25)(H,22,23)(H2,21,24,27);2,4H,1H3,(H,5,6)/t;2-/m.0/s1

HIDE SMILES / InChI

Description
Curator's Comment: Description was created based on several sources, including https://www.drugbank.ca/drugs/DB05169 https://www.ncbi.nlm.nih.gov/pubmed/21154126

AT-9283 was being developed by Astex Pharmaceuticals as a treatment for cancer and myelofibrosis. AT-9283 is an inhibitor of mitosis (cell division) and is the second most progressed drug candidate in the Astex portfolio of novel molecularly targeted cancer drugs. All of Astex’s current products have been discovered internally using its proprietary drug discovery approach. AT9283 is a potent inhibitor of the Aurora A and B kinases and has been shown to arrest tumour growth in a range of tumour models. Aurora kinases play a key role in mitotic checkpoint control in cell division. Both Aurora A and B are over-expressed in many human tumours and are believed to be excellent targets for anti-cancer therapy.

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
19.1 ng/mL
6 mg/m² 72 times / hour multiple, intravenous
dose: 6 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
AT-9283 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
25.4 ng/mL
9 mg/m² 72 times / hour multiple, intravenous
dose: 9 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
AT-9283 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
4.7 ng/mL
1.5 mg/m² 72 times / hour multiple, intravenous
dose: 1.5 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
AT-9283 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
42.9 ng/mL
13 mg/m² 72 times / hour multiple, intravenous
dose: 13 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
AT-9283 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
1653 ng × h/mL
51.3 mg 72 times / hour multiple, intravenous
dose: 51.3 mg
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
AT-9283 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
20956 ng × h/mL
567 mg 72 times / hour multiple, intravenous
dose: 567 mg
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
AT-9283 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
1200 ng × h/mL
6 mg/m² 72 times / hour multiple, intravenous
dose: 6 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
AT-9283 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1720 ng × h/mL
9 mg/m² 72 times / hour multiple, intravenous
dose: 9 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
AT-9283 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
278 ng × h/mL
1.5 mg/m² 72 times / hour multiple, intravenous
dose: 1.5 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
AT-9283 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
2910 ng × h/mL
13 mg/m² 72 times / hour multiple, intravenous
dose: 13 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
AT-9283 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
2984 ng × h/mL
67.7 mg 72 times / hour multiple, intravenous
dose: 67.7 mg
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
AT-9283 plasma
Homo sapiens
population: UNHEALTHY
age: CHILD
sex: UNKNOWN
food status: UNKNOWN
38254 ng × h/mL
500 mg 72 times / hour multiple, intravenous
dose: 500 mg
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
AT-9283 plasma
Homo sapiens
population: UNHEALTHY
age: CHILD
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
7.6 h
6 mg/m² 72 times / hour multiple, intravenous
dose: 6 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
AT-9283 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
7.8 h
9 mg/m² 72 times / hour multiple, intravenous
dose: 9 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
AT-9283 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
13.4 h
1.5 mg/m² 72 times / hour multiple, intravenous
dose: 1.5 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
AT-9283 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
7.5 h
13 mg/m² 72 times / hour multiple, intravenous
dose: 13 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
AT-9283 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Patents

Sample Use Guides

Starting dose will be 40 mg/m2/day OR 30 mg/m2/day to be confirmed at registration. IV 24 hour continuous infusion Days 1 and 8 every three weeks
Route of Administration: Intravenous
AT-9283 leads to a clear polyploid phenotype by inhibiting the activity of Aurora B kinase in HCT116 cells with IC50 of 30 nM. Furthermore, AT-9283 also produces the potent inhibition on HCT116 colony formation.
Name Type Language
AT-9283 L-LACTATE
Code English
PROPANOIC ACID, 2-HYDROXY-, (2S)-, COMPD. WITH N-CYCLOPROPYL-N'-(3-(6-(4-MORPHOLINYLMETHYL)-1H-BENZIMIDAZOL-2-YL)-1H-PYRAZOL-4-YL)UREA (1:1)
Systematic Name English
Code System Code Type Description
CAS
896466-76-5
Created by admin on Fri Dec 15 16:21:31 GMT 2023 , Edited by admin on Fri Dec 15 16:21:31 GMT 2023
PRIMARY
PUBCHEM
135566103
Created by admin on Fri Dec 15 16:21:31 GMT 2023 , Edited by admin on Fri Dec 15 16:21:31 GMT 2023
PRIMARY
EPA CompTox
DTXSID20635838
Created by admin on Fri Dec 15 16:21:31 GMT 2023 , Edited by admin on Fri Dec 15 16:21:31 GMT 2023
PRIMARY
FDA UNII
NP03YG4TOE
Created by admin on Fri Dec 15 16:21:31 GMT 2023 , Edited by admin on Fri Dec 15 16:21:31 GMT 2023
PRIMARY