Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C26H29N7O2 |
| Molecular Weight | 471.5542 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@H]1CC[C@@H](CC1)N2C3=NC(NC4=NC5=C(CN(CC5)C(=O)CO)C=C4)=NC=C3C6=C2C=NC=C6
InChI
InChIKey=BBUVDDPUURMFOX-SAABIXHNSA-N
InChI=1S/C26H29N7O2/c1-16-2-5-18(6-3-16)33-22-13-27-10-8-19(22)20-12-28-26(31-25(20)33)30-23-7-4-17-14-32(24(35)15-34)11-9-21(17)29-23/h4,7-8,10,12-13,16,18,34H,2-3,5-6,9,11,14-15H2,1H3,(H,28,29,30,31)/t16-,18-
| Molecular Formula | C26H29N7O2 |
| Molecular Weight | 471.5542 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
DescriptionCurator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/24526162
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/24526162
AMG-925, a dual FLT3/CDK4 inhibitor, has been developed to overcome resistance to FLT3 inhibitors, which is a serious clinical issue in treating acute myelogenous leukemia (AML). AMG-925 inhibits FLT3, including many FLT3 mutants reported to date. AMG-925 inhibits the proliferation of a panel of human tumor cell lines including Colo205 (Rb(+)) and U937 (FLT3(WT)) and induced cell death in MOLM13 (FLT3(ITD)) and even in MOLM13 (FLT3(ITD, D835Y)), which exhibits resistance to a number of FLT3 inhibitors currently under clinical development. At well-tolerated doses, AMG-925 leads to significant growth inhibition of MOLM13 xenografts in nude mice, and the activity correlates with inhibition of STAT5 and Rb phosphorylation. AMG-925 is in Phase I clinical trials for the treatment of Acute myeloid leukaemia.
Originator
Approval Year
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 08:54:08 UTC 2023
by
admin
on
Sat Dec 16 08:54:08 UTC 2023
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| Record UNII |
RB6Y814V4I
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| Record Status |
Validated (UNII)
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| Record Version |
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145537
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1401033-86-0
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60202647
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RB6Y814V4I
Created by
admin on Sat Dec 16 08:54:08 UTC 2023 , Edited by admin on Sat Dec 16 08:54:08 UTC 2023
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