BMS-833923

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Chemical Structure| 1059734-66-5 同义名 : XL-139
CAS号 : 1059734-66-5
货号 : A174690
分子式 : C30H27N5O
纯度 : 98%
分子量 : 473.57
MDL号 : MFCD25976660
存储条件：

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 The Hedgehog (Hh) pathway plays an important role in embryonic development and adult tissue maintenance via the regulation of cell differentiation and proliferation. Smoothened (Smo), a member of the GPCR superfamily, belongs to class F (Frizzled family) and is the main transducer of the Hh signaling pathway. BMS-833923 (XL 139) is an inhibitor of Smoothened with potential antineoplastic activity. Esophageal adenocarcinoma (EAC) cell lines OE19 and OE33 treated with 10 μM and 25 μM BMS-833923 showed 50% and 100% cell death, and caspase-3 was activated in 25 μM BMS-833923-treated group. Hh targeted gene Gli1 in the nuclear fraction was significantly decreased in both cell lines treated with 10 μM BMS-833923 compared to untreated cells[3]. BMS-833923 (30 mg/kg) monotherapy for 7 days in nu/nu mice xenograft model of cholangiocarcinoma resulted in a reduction of tumor volume (60% ± 23%) but the most pronounced size reduction could be seen in the gemcitabine (40 mg/kg)/BMS-833923 combination group (32% ± 5%)[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.11mL

0.42mL

0.21mL

10.56mL

2.11mL

1.06mL

21.12mL

4.22mL

2.11mL
参考文献

[1]Wilkinson SE, Furic L, et al. Hedgehog signaling is active in human prostate cancer stroma and regulates proliferation and differentiation of adjacent epithelium. Prostate. 2013 Dec;73(16):1810-23.

[2]Zaidi AH, Komatsu Y, et al. Smoothened inhibition leads to decreased proliferation and induces apoptosis in esophageal adenocarcinoma cells. Cancer Invest. 2013 Aug;31(7):480-9.

[3]Zaidi AH, Komatsu Y, Kelly LA, Malhotra U, Rotoloni C, Kosovec JE, Zahoor H, Makielski R, Bhatt A, Hoppo T, Jobe BA. Smoothened inhibition leads to decreased proliferation and induces apoptosis in esophageal adenocarcinoma cells. Cancer Invest. 2013 Aug;31(7):480-9. doi: 10.3109/07357907.2013.820317. PMID: 23915072.

[4]Riedlinger D, Bahra M, Boas-Knoop S, Lippert S, Bradtmöller M, Guse K, Seehofer D, Bova R, Sauer IM, Neuhaus P, Koch A, Kamphues C. Hedgehog pathway as a potential treatment target in human cholangiocarcinoma. J Hepatobiliary Pancreat Sci. 2014 Aug;21(8):607-15. doi: 10.1002/jhbp.107. Epub 2014 Apr 15. PMID: 24733827.