BCL-201 dihydrochloride
- Servier 1 dihydrochloride
- Parent CAS: 1448584-12-0
- Optical Purity: 99% e.e.
- Soluble in DMSO
- MF: C43H42N4O6.2HCl
- MW: 783.74
Description
BCL-201 (S55746, Servier-1) is an orally bioavailable, potent and selective BH3-mimetic inhibitor of BCL-2 protein with a Ki of 1.3 nM, highly selective over BCL-XL (70- 400 fold), and no significant binding to MCL-1 and BFL-1 (BCL2A1/A1). BCL-201 induces hallmarks of apoptosis including externalization of phosphatidylserine, caspase-3 activation and PARP cleavage. Ex vivo, it induces apoptosis in the low nanomolar range in primary Chronic Lymphocytic Leukemia and Mantle Cell Lymphoma patient samples. Finally, BCL-201 (S55746) administered by oral route daily in mice demonstrated robust anti-tumor efficacy in two hematological xenograft models with no weight lost and no change in behavior.
More Information
| Parent CAS No. | 1448584-12-0 |
|---|---|
| Chemical Name | (S)-N-(4-hydroxyphenyl)-3-(6-(3-(morpholinomethyl)-1,2,3,4-tetrahydroisoquinoline-2-carbonyl)benzo[d][1,3]dioxol-5-yl)-N-phenyl-5,6,7,8-tetrahydroindolizine-1-carboxamide dihydrochloride |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C12CN(C(C3C=C4OCOC4=CC=3C3=CC(C(=O)N(C4C=CC(O)=CC=4)C4C=CC=CC=4)=C4CCCCN34)=O)[C@H](CN3CCOCC3)CC=1C=CC=C2.Cl.Cl |&1:39,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C43H42N4O6/c48-34-15-13-32(14-16-34)47(31-10-2-1-3-11-31)43(50)37-23-39(45-17-7-6-12-38(37)45)35-24-40-41(53-28-52-40)25-36(35)42(49)46-26-30-9-5-4-8-29(30)22-33(46)27-44-18-20-51-21-19-44/h1-5,8-11,13-16,23-25,33,48H,6-7,12,17-22,26-28H2/t33-/m0/s1 |
| InChiKey | VYXJULKGMXJVGI-XIFFEERXSA-N |
| CID | 71654876 |
| Short Description | BH3-mimetic inhibitor of BCL-2 protein |
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