产品名称

英文名称：BMS-833923

同义词

BMS-833923、1059734-66-5、BMS 833923、N-(2-Methyl-5-((methylamino)methyl)phenyl)-4-((4-phenylquinazolin-2-yl)amino)benzamide、XL139、BMS833923、BMS-833923 (XL-139)、XL-139、BMS-833923 free base anhydrous、XL 139、41J7ZJ239R、N-[2-methyl-5-(methylaminomethyl)phenyl]-

产品性质

CAS编号：1059734-66-5

分子式：C30H27N5O

分子量：473.57

PubChem编号：57662985

英文别名：BMS-833923|1059734-66-5|BMS 833923|N-(2-Methyl-5-((methylamino)methyl)phenyl)-4-((4-phenylquinazolin-2-yl)amino)benzamide|XL139|BMS833923|BMS-833923 (XL-139)|XL-139|BMS-833923 free base anhydrous|XL 139|41J7ZJ239R|N-[2-methyl-5-(methylaminomethyl)phenyl]-

规格或纯度：98%

英文名称：BMS-833923

生化机理：DescriptionIC50 Value 6-35 nM [1]BMS-833923 (or XL-139) is an orally bioavailable small-molecule SMO (Smoothened) inhibitor with potential antineoplastic activity. SMO antagonist BMS-833923 inhibits the sonic hedgehog (SHH) pathway protein SMO, which may result in a suppression of the SHH signaling pathway.in vitro In vitro, BMS-833923 inhibits the expression of downstream effectors in the HH pathway (GLI1 and PTCH1) in cell lines that express wild-type SMO and those which express activated mutant forms of SMO (IC50values of 6-35 nM). In FACS-based binding assays, BMS-833923 inhibits BODIPY cyclopamine binding to SMO in a dose-dependent manner with an IC50 of 21 nM [1].in vivo Pharmacodynamic studies show that BMS-833923 robustly inhibits HH pathway activity with along duration of action after a single oral dose in medulloblastoma and pancreatic carcinoma xenograft models. The pharmacodynamic effects of BMS-833923 observed in these models translate into tumor growth inhibition at well-tolerated doses [1].Clinical trial Dasatinib Combo With Smoothened (SMO) Antagonist (BMS-833923). Phase 2.Potent Smoothened antagonist (IC 50 = 5.8 nM). Blocks Hedgehog signaling in cell-based assays. Inhibits Gli1 and PTCH1 expression in cell lines. Reduces proliferation and induces apoptosis in tumor cellls.

储存温度：-20°C储存

运输条件：超低温冰袋运输

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ALogP：5.7

IUPAC Name：N-[2-methyl-5-(methylaminomethyl)phenyl]-4-[(4-phenylquinazolin-2-yl)amino]benzamide

INCHI：InChI=1S/C30H27N5O/c1-20-12-13-21(19-31-2)18-27(20)33-29(36)23-14-16-24(17-15-23)32-30-34-26-11-7-6-10-25(26)28(35-30)22-8-4-3-5-9-22/h3-18,31H,19H2,1-2H3,(H,33,36)(H,32,34,35)

InChi Key：KLRRGBHZCJLIEL-UHFFFAOYSA-N

Canonical SMILES：CC1=C(C=C(C=C1)CNC)NC(=O)C2=CC=C(C=C2)NC3=NC4=CC=CC=C4C(=N3)C5=CC=CC=C5

Isomeric SMILES：CC1=C(C=C(C=C1)CNC)NC(=O)C2=CC=C(C=C2)NC3=NC4=CC=CC=C4C(=N3)C5=CC=CC=C5

PubChem CID：57662985

CAS Registry No.：1059734-66-5

溶解性：DMSO 95 mg/mL Water <1 mg/mL Ethanol <1 mg/mL

产品包装