A-1210477
- Soluble in DMSO
- MF: C46H55N7O7S
- MW: 850.04
Description
A-1210477 is a proteolytically stable, cell-permeable and high affinity BH3 mimetics of anti-apoptotic protein MCL-1, binding to the target potently and selectively with a Ki value of 0.45 nM, highly selective against closely related proteins of BCL-2 (Ki = 132 nM, >290-fold selectivity) and BCL-XL (Ki > 660 nM, >1400-fold selectivity). A-1210477 is the first-in-class small molecule MCL-1 inhibitor with sufficient potency to disrupt the tight-binding MCL-1-BIM complex in living cells, achieving the hallmarks of intrinsic apoptosis, and demonstrating clear-on-target cancer cell killing capability either as a single agent or in combination with ABT-263 (Axon 3821).
More Information
| Parent CAS No. | 1668553-26-1 |
|---|---|
| Chemical Name | 7-(5-((4-(4-(N,N-Dimethylsulfamoyl)piperazin-1-yl)phenoxy)methyl)-1,3-dimethyl-1H-pyrazol-4-yl)-1-(2-morpholinoethyl)-3-(3-(naphthalen-1-yloxy)propyl)-1H-indole-2-carboxylic acid |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C1C=C2C(CCCOC3C=CC=C4C=CC=CC=34)=C(C(=O)O)N(CCN3CCOCC3)C2=C(C2C(C)=NN(C)C=2COC2C=CC(N3CCN(S(=O)(=O)N(C)C)CC3)=CC=2)C=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C46H55N7O7S/c1-33-43(41(49(4)47-33)32-60-36-19-17-35(18-20-36)51-22-24-52(25-23-51)61(56,57)48(2)3)40-14-8-13-38-39(15-9-29-59-42-16-7-11-34-10-5-6-12-37(34)42)45(46(54)55)53(44(38)40)26-21-50-27-30-58-31-28-50/h5-8,10-14,16-20H,9,15,21-32H2,1-4H3,(H,54,55) |
| InChiKey | XMVAWGSQPHFXKU-UHFFFAOYSA-N |
| CID | 66575373 |
| Short Description | Mcl-1 inhibitor |
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