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Merck
CN

SML2436

BAY-958 hydrochloride

≥98% (HPLC)

别名:

(3-((4-(4-Fluoro-2-methoxyphenyl)-1,3,5-triazin-2-yl)amino)phenyl)methanesulfonamide hydrochloride, 3-[[4-(4-Fluoro-2-methoxyphenyl)-1,3,5-triazin-2-yl]amino]benzenemethanesulfonamide hydrochloride, BAY 958 HCl, BAY958 HCl, LDC 526 HCl, LDC526 HCl

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关于此项目

经验公式(希尔记法):
C17H16FN5O3S · HCl
化学文摘社编号:
分子量:
425.86
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
powder
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assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

FC1=CC=C(C2=NC(NC3=CC(CS(=O)(N)=O)=CC=C3)=NC=N2)C(OC)=C1.Cl

InChI key

WKPVFIKSRZVXOX-UHFFFAOYSA-N

Biochem/physiol Actions

BAY-958 (LDC526) is an orally active, ATP site-targeting, potent and selective PTEFb/CDK9 inhibitor (hCDK9-CycT1 IC50 = 5-11 nM; [ATP] = 10 μM) with 52- to >2000-fold selectivity over CDK1-7 with antiproliferative activity in cancer cultures (IC50 = 0.28 μM/96h/MOLM-13, 1 μM/96h/HeLa, 0.55 μM/48h/MEC-1, 0.28 μM/48h/CCL patient PBMCs). When administered orally in mice, BAY-958 significantly suppresses MOLM-13 acute myeloid leukemia (AML) tumor growth in mice (30/40 mg/kg/day p.o.; HCl salt) and exhibits in vivo efficacy in two murine chronic lymphocytic leukemia (CLL) models (50 & 70 mg/kg/day p.o.; free base).
Orally active, ATP site-targeting, potent and selective PTEFb/CDK9 inhibitor with anti-cancer efficacy in vitro and in vivo.


存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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