S55746
- Product Name
- S55746
- CAS No.
- 1448584-12-0
- Chemical Name
- S55746
- Synonyms
- BLC201;S55746;S55746 (BLC201);BCL-201 (S55746);S55746, 10 mM in DMSO;S55746(S055746,BCL201);S55746 (Synonyms: BLC201);inhibit,BCL-201,Inhibitor,Bcl-2 Family,S55746,S-55746,BCL 201,BCL201,S 55746;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;(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
- CBNumber
- CB74668476
- Molecular Formula
- C43H42N4O6
- Formula Weight
- 710.82
- MOL File
- 1448584-12-0.mol
S55746 Property
- 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 and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- DC12163
- Product name
- S55746(BLC201)
- Purity
- >98%
- Packaging
- 100mg
- Price
- $1300
- Updated
- 2021/12/16
S55746 Chemical Properties,Usage,Production
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
S55746 Preparation Products And Raw materials
Raw materials
Preparation Products
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