您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > BMS-833923(XL-139)
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
BMS-833923(XL-139)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BMS-833923(XL-139)图片
CAS NO:1059734-66-5
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)473.57
FormulaC30H27N5O
CAS No.1059734-66-5
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 95 mg/mL (200.6 mM)
Water:<1 mg/mL
Ethanol: <1 mg/mL
SMILESO=C(NC1=CC(CNC)=CC=C1C)C2=CC=C(NC3=NC(C4=CC=CC=C4)=C5C=CC=CC5=N3)C=C2
SynonymsXL139; BMS833923; XL-139; BMS-833923; BMS 833923; XL 139.
实验参考方法
In Vitro

In vitro activity: BMS-833923 reduces hedgehog pathway activity, decreases cell proliferation and induces apoptosis via the intrinsic pathway in esophageal adenocarcinoma (EAC) cell lines. BMS-833923 dose-dependently affects canonical and prostate hedgehog signature gene transcription in vitro.


Kinase Assay: BMS-833923 (XL-139) is an orally bioavailable small-molecule inhibitor of Smoothened with potential antineoplastic activity; inhibits BODIPY cyclopamine binding to SMO in a dose-dependent manner with an IC50 of 21 nM.


Cell Assay: BMS-833923 inhibited the expression of GLI1 and PTCH1 in cell lines expressing wild-type SMO or activated mutant SMO with IC50 values in the range from 6 to 35 nM. In the FACS-based binding assays, it does-dependently suppressed cyclopamine binding to SMO with IC50 value of 21 nM. In the esophageal adenocarcinoma cell lines OE19 and OE33, treatment of BMS-833923 significantly reduced cell proliferation with IC50 values of both 10 μM. Besides that, BMS-833923 was found to inhibit the growth of multiple myeloma cells and the proportion of ALDH+ cancer stem cells. It also inhibited the growth of many other tumor cells derived from patients with hematological malignancies including ALL, AML and CM.

In VivoIn animal models with medulloblastoma and pancreatic carcinoma xenografts, administration of BMS-833923 at single oral dose showed robust inhibition of Hh pathway. In a rat model with gastroesophageal reflux disease, the administration of BMS-833923 at dose of 10 mg/kg/day resulted in the decreased development of both Barrett esophagus and esophageal adenocarcinoma by 35.7%.
Animal modelAnimal models with medulloblastoma and pancreatic carcinoma xenografts
Formulation & Dosage10 mg/kg/day; oral
ReferencesCancer Invest. 2013 Aug;31(7):480-9; Prostate. 2013 Dec;73(16):1810-23.