NVP-CGM097 dihydrochloride
- CGM097 dihydrochloride
- Parent CAS: 1313363-54-0
- Optical Purity: 99% e.e.
- Soluble in DMSO
- MF: C38H47ClN4O4.2HCl
- MW: 730.28
Description
NVP-CGM097 dihydrochloride is a potent and selective MDM2 inhibitor. Optically pure (S-Enantiomer) NVP-CGM097 binds to the p53 binding-site of the Human MDM2 protein with an IC50 value of 1.7 nM, highly selective against other protein-protein interactions such as p53:MDM4 (>1000-fold selectivity), Ras:Raf (3000-fold selectivity), and showing no significant activity against Bcl-2:Bak, Bcl-2:Bad, Mcl-1:Bak, Mcl-1:NOXA, XIAP:BIR3, and c-IAP:BIR3 protein−protein interactions. It inhibits the p53:MDM2 interaction in cells, leading to p53 nuclear translocation that results in cell growth inhibition in a p53-dependent manner. Exhibit excellent in vivo pharmacological properties. The parent compound NVP-CGM097 is available as Axon 3751.
More Information
| Parent CAS No. | 1313363-54-0 |
|---|---|
| Chemical Name | (S)-1-(4-chlorophenyl)-7-isopropoxy-6-methoxy-2-(4-(methyl(((1r,4r)-4-(4-methyl-3-oxopiperazin-1-yl)cyclohexyl)methyl)amino)phenyl)-1,2-dihydroisoquinolin-3(4H)-one dihydrochloride |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C1C2[C@H](C3C=CC(Cl)=CC=3)N(C3C=CC(N(C[C@@H]4CC[C@@H](N5CCN(C)C(=O)C5)CC4)C)=CC=3)C(=O)CC=2C=C(OC)C=1OC(C)C.Cl.Cl |&1:2,17,20,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C38H47ClN4O4/c1-25(2)47-35-22-33-28(20-34(35)46-5)21-36(44)43(38(33)27-8-10-29(39)11-9-27)32-16-14-30(15-17-32)41(4)23-26-6-12-31(13-7-26)42-19-18-40(3)37(45)24-42/h8-11,14-17,20,22,25-26,31,38H,6-7,12-13,18-19,21,23-24H2,1-5H3/t26?,31?,38-/m0/s1 |
| InChiKey | CLRSLRWKONPSRQ-CPOWQTMSSA-N |
| CID | 53240420 |
| Short Description | MDM2 inhibitor |
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