BMS-833923,BMS-833923
  • BMS-833923,BMS-833923

1059734-66-5BMS-833923

价格 询价
包装 1盒
最小起订量 1盒
发货地 上海
更新日期 2024-11-01
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产品详情

中文名称:BMS-833923英文名称:BMS-833923
CAS:1059734-66-5品牌: 一研
保存条件: Store at -20°C产品类别: 抑制剂
Cas : 1059734-66-5
2024-11-01 BMS-833923 BMS-833923 1盒/RMB 一研 Store at -20°C 抑制剂

产品属性:

产品名称

规格

CAS

型号

BMS-833923

5mg 10mg 50mg

1059734-66-5

EY-Y0165444

Cas No.1059734-66-5

别名 BMS 833923;BMS833923;XL-139;XL139;XL 139

化学名 N-[2-methyl-5-(methylaminomethyl)phenyl]-4-[(4-phenylquinazolin-2-yl)amino]benzamide

分子式 C30H27N5O

BMS-833923.png

分子量 473.57

溶解度 47.4 mg/mL in DMSO, 5.14 mg/mL in EtOH with ultrasonic and warming

储存条件 Store at -20°C
General tips  For obtaining a higher solubility , please warm the tube at 37 and shake it in the ultrasonic bath for a while.
Shipping Condition     Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述:
The Hedgehog (Hh) signaling is a critical pathway involved in embryonic development and in tissue maintenance and repair in adults. It consists of the Hh ligands, the transmembrane receptors Patched 1 and 2, the G-protein- coupled receptor-like protein SMO and the glioma-associated oncogene transcription factors GLI1 to 3. The aberrant activation of Hh pathway, both mutational and epigenetic, is found to be associated with multiple aspects of tumorigenesis in various tumor cells. As a smoothened inhibitor, BMS-833923 can block the binding of cyclopamine (a naturally occurring SMO inhibitor) to SMO. It showed potent Hh pathway inhibitory activity with IC50 values at nanomolar in multiple cell-based assays. BMS-833923 also potently inhibited Hh pathway in medulloblastoma and pancreatic carcinoma xenograft models [1, 2 and 3].

In vitro, 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 CML [3 and 4].

In 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% [3 and 5].

References:

[1] Siu L L, Papadopoulos K P, Alberts S, et al. A first-in-human phase 1study of an oral hedgehog pathway antagonist, BMS-833923 (XL139), in subjects with advanced or metastatic solid tumors. Mol Cancer Ther, 2009, 8(12 Suppl): A55.

[2] Justilien V, Fields A P. Molecular Pathways: Novel Approaches for Improved Therapeutic Targeting of Hedgehog Signaling in Cancer Stem Cells. Clinical Cancer Research, 2015, 21(3): 505-513.

[3] Gendreau S B, Hawkins D, Ho C P, et al. Abstract B192: Preclinical characterization of BMS833923 (XL139), a hedgehog (HH) pathway inhibitor in early clinical development. Molecular Cancer Therapeutics, 2009, 8(12 Supplement): B192-B192.

[4] Zaidi A H, Komatsu Y, Kelly L A, et al. Smoothened inhibition leads to decreased proliferation and induces apoptosis in esophageal adenocarcinoma cells. Cancer investigation, 2013, 31(7): 480-489.

[5] Gibson M K, Zaidi A H, Davison J M, et al. Prevention of Barrett esophagus and esophageal adenocarcinoma by smoothened inhibitor in a rat model of gastroesophageal reflux disease. Annals of surgery, 2013, 258(1): 82-88.


关键字: 1059734-66-5;C30H27N5O;BMS-833923;

公司简介

上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要从事免疫学、分子生物学和常规生化试剂等为一体的科研产品销售企业,公司自成立以来,秉承""全心全意服务于科研工作者""的企业理念,立足生物科技领域,运用生物技术和科研试剂,发展现代生物科技,为各类大中小医院及其它医疗机构、高等院校、科研院所、企事业单位提供优质的产品,服务生物科技领域的科学研究人员。 公司具有对普通货物、冷藏及冷冻仓库的存储、包装及运输能力。 公司将始终坚持信誉立业、以人为本、质量保证、诚信服务的宗旨,不断拼搏,开拓进取,与各界朋友携手共创美好未来。
成立日期 2014-06-05 (11年) 注册资本 100
员工人数 50-100人 年营业额 ¥ 100万以内
主营行业 生化试剂,抗体,细胞培养,分子生物学,免疫安全 经营模式 工厂,试剂
  • 上海一研生物科技有限公司
VIP 2年
  • 公司成立:11年
  • 注册资本:100
  • 企业类型:营业执照
  • 主营产品:、ELISA试剂盒、PCR检测试剂盒、生化检测试剂盒、标准品、抗体、细胞等
  • 公司地址:上海市闵行区莘福路2号楼
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