| Identification | Back Directory | [Name]
S55746 | [CAS]
1448584-12-0 | [Synonyms]
S55746
BLC201
S55746 (BLC201)
S55746(S055746,BCL201)
S55746 (Synonyms: BLC201)
N-(4-hydroxyphenyl)-3-[6-[(3S)-3-(morpholin-4-ylmethyl)-3,4-dihydro-1H-isoquinoline-2-carbonyl]-1,3-benzodioxol-5-yl]-N-phenyl-5,6,7,8-tetrahydroindolizine-1-carboxamide
1-Indolizinecarboxamide, 3-[6-[[(3S)-3,4-dihydro-3-(4-morpholinylmethyl)-2(1H)-isoquinolinyl]carbonyl]-1,3-benzodioxol-5-yl]-5,6,7,8-tetrahydro-N-(4-hydroxyphenyl)-N-phenyl- | [Molecular Formula]
C43H42N4O6 | [MDL Number]
MFCD31715456 | [MOL File]
1448584-12-0.mol | [Molecular Weight]
710.82 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 50 mg/mL (70.34 mM);Water : < 0.1 mg/mL (insoluble) | [form ]
Solid | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
S55746 (Bcl201, Servier-1) is orally available and has been reported to effectively kill cancer cells that overexpress Bcl-2 using both in vitro and in vivo models. Currently, S55746 as a single agent is in phase-I trials in relapsed or refractory CLL patients. As a sensitizing agent, S55746 is currently being tested for a combination use with PI3Kδinhibitor for follicular lymphoma and mantle cell lymphoma. | [Uses]
S55746 (BCL201) is a potent, orally active and selective BCL-2 inhibitor, with a Ki of 1.3 nM and a Kd of 3.9 nM. S55746 (BCL201) has antitumor activity with low toxicity[1]. | [in vivo]
S55746 is a highly efficacious and well-tolerated (even at doses up to 300 mg/kg) orally active BCL-2 inhibitor[1].
S55746 (20-100 mg/kg, p.o.) inhibits xenograft growth in RS4;11 and Toledo models time- and dose-dependently[1]. | Animal Model: | Female SCID/beige mice implanted subcutaneously with 3×106 Toledo or RS4;11[1]. | | Dosage: | 20, 50, 100 mg/kg. | | Administration: | Oral gavage daily for 7 consecutive days. | | Result: | Induced significant anti-tumor activity time- and dose-dependently. |
| Animal Model: | SCID/beige female mice with RS4;11 tumor xenografts[1]. | | Dosage: | 25 and 100 mg/kg. | | Administration: | Single oral gavage treatment. | | Result: | Did not induce platelet loss in vivo at 25 and 100 mg/kg. |
| [IC 50]
Bcl-2: 1.3 nM (Ki); Bcl-xL: 520 nM (Ki); Bcl-2: 3.9 nM (Kd); Bcl-xL: 186 nM (Kd) | [References]
[1] Casara P, et al. S55746 is a novel orally active BCL-2 selective and potent inhibitor that impairs hematological tumor growth. Oncotarget. 2018 Apr 13;9(28):20075-20088. DOI:10.18632/oncotarget.24744 |
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| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
cjbscvictory
|
| Tel: |
13348960310 13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
|