BCL-201 dihydrochloride - Servier 1 dihydrochloride

Based on 11 reference(s) in Google Scholar 8 10 11

Axon 3714

CAS [N.A.]

MF C43H42N4O6.2HCl
MW 783.74

  • Purity: 99%
  • Optical purity: 99%
  • Soluble in DMSO
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BCL-201 dihydrochloride

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.

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KEYWORDS: BCL-201 dihydrochloride | BH3-mimetic inhibitor of BCL-2 protein | Servier 1 dihydrochloride | BCL201 | BCL 201 | S-55746 | S 55746 | CT-BCL201 | CAS [N.A.] | [1448584-12-0] | Non Selective | Bcl | Inhibitor | Proteins

BH3-mimetic inhibitor of BCL-2 protein

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

Source information

Sold in collaboration with Chemietek

Parent CAS No.

[1448584-12-0]

The purity of Axon Ligands™ is confirmed by HPLC-MS, 1H-NMR and/or microanalysis. Analytical data are available upon request.

Caution: Axon Ligands™ are not fully tested. They are for research purposes only! Not for human consumption!

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