Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C25H26ClN5O3 |
| Molecular Weight | 479.959 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=C2N=C(NC2=CC(=C1)N3CCOCC3)C4=C(NC[C@@H](O)C5=CC=CC(Cl)=C5)C=CNC4=O
InChI
InChIKey=ZWVZORIKUNOTCS-OAQYLSRUSA-N
InChI=1S/C25H26ClN5O3/c1-15-11-18(31-7-9-34-10-8-31)13-20-23(15)30-24(29-20)22-19(5-6-27-25(22)33)28-14-21(32)16-3-2-4-17(26)12-16/h2-6,11-13,21,32H,7-10,14H2,1H3,(H,29,30)(H2,27,28,33)/t21-/m1/s1
DescriptionCurator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/19789352
https://www.ncbi.nlm.nih.gov/pubmed/19258511
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/19789352
https://www.ncbi.nlm.nih.gov/pubmed/19258511
BMS-536924 is an ATP-competitive IGF-1R/IR inhibitor with IC50 of 100 nM/73 nM, modest activity for Mek, Fak, and Lck with very little activity for Akt1, MAPK1/2. BMS-536924 has been shown to inhibit the catalytic activity of IGF-1R and its down stream signaling components such as Akt and MAPK in cells; it also inhibits proliferation in a wide variety of human cancer cell lines including, colon, breast, lung, pancreas, prostate, sarcoma and multiple myeloma. In vivo, BMS-536924 inhibits tumor growth in an IGF-1R-dependent tumor model (IGF-1R Sal) as well as in a broad range of human tumor xenografts.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL395 |
|||
Target ID: CHEMBL1981 |
73.0 nM [IC50] | ||
| 100.0 nM [IC50] | |||
Target ID: CHEMBL2695 |
150.0 nM [IC50] | ||
Target ID: CHEMBL387 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
|||
| Primary | Unknown Approved UseUnknown |
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| Primary | Unknown Approved UseUnknown |
PubMed
| Title | Date | PubMed |
|---|---|---|
| In-vitro growth inhibition of chemotherapy and molecular targeted agents in hepatocellular carcinoma. | 2013 Mar |
|
| The effect of IGF-I receptor blockade for human esophageal squamous cell carcinoma and adenocarcinoma. | 2014 Feb |
|
| BMS-536924, an ATP-competitive IGF-1R/IR inhibitor, decreases viability and migration of temozolomide-resistant glioma cells in vitro and suppresses tumor growth in vivo. | 2015 |
Sample Use Guides
Mice: oral administration of 70 mg/kg BMS-536924 significantly inhibits tumor growth (TGBC-1TKB cells) inoculated in nude mice.
Route of Administration:
Oral
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468740-43-4
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40E3AZG1MX
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135440466
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ACTIVE MOIETY
