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MedChemExpress - Model BMS-833923 - ...

MedChemExpress - Model BMS-833923 - 1059734-66-5

BMS-833923 (XL-139) is an orally biocompatible Smoothened (Smo) inhibitor with anti-tumor activity. It can inhibit the binding of BODIPY cyclopamine to SMO in a dose-dependent manner with an IC50 of 21 nM[1].

BMS-833923

MCE China：BMS-833923

Brand：MedChemExpress (MCE)

Cat. No.HY-13809

CAS：1059734-66-5

Synonyms：XL-139

Purity：99.82%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：BMS-833923 (XL-139) is an orally biocompatible Smoothened (Smo) inhibitor with anti-tumor activity. It can inhibit the binding of BODIPY cyclopamine to SMO in a dose-dependent manner with an IC50 of 21 nM.

In Vitro：BMS‐833923 inhibits the expression of downstream effectors in the HH pathway (GLI1 and PTCH1) wild‐type SMO and activated mutant forms of SMO expressing cells (IC50: 6-35 nM)[1]. BMS‐833923 (2.5-10 μM, 48 h) inhibits cell proliferation of both A549 and H1299 cells[2]. BMS‐833923 (3 µM) inhibits osteoblast differentiation and mineralization of hMSCs, determined by decreased ALP activity and downregulation of osteoblast-related gene expression[3].

In Vivo：BMS-833923 (15 mg/kg, oral gavage, daily) alone or together with Selumetinib (HY-50706) (10 mg/kg, oral gavage, daily) reduces tumor metastasis and the post-extravasation tumor growth in orthotopic mouse model of pancreatic cancer metastasis[4]. BMS-833923 (30 mg/kg, p.o., seven consecutive days) alone or together with Gemcitabine (HY-17026) (40 mg/kg, i.p., at the 1st, 4th and 7th day) reduces tumor volume (to 60% and 32% respectively) in a nu/nu mice xenograft model of cholangiocarcinoma[5].

References：

[1]. Steven B, et al. Abstract B192: Preclinical characterization of BMS-833923 (XL139), a hedgehog (HH) pathway inhibitor in early clinical development. Molecular Cancer Therapeutics: December 2009; Volume 8, Issue 12, Supplement 1.

[2]. Du J, et al. Disruption of SHH signaling cascade by SBE attenuates lung cancer progression and sensitizes DDP treatment. Sci Rep. 2017 May 15;7(1):1899. [Content Brief]

[3]. AlMuraikhi N, et al. Hedgehog Signaling Inhibition by Smoothened Antagonist BMS-833923 Reduces Osteoblast Differentiation and Ectopic Bone Formation of Human Skeletal (Mesenchymal) Stem Cells. Stem Cells Int. 2019 Nov 21;2019:3435901. [Content Brief]

[4]. Gu D, et al. Simultaneous Inhibition of MEK and Hh Signaling Reduces Pancreatic Cancer Metastasis. Cancers (Basel). 2018 Oct 26;10(11):403. [Content Brief]

[5]. Riedlinger D, et al. Hedgehog pathway as a potential treatment target in human cholangiocarcinoma. J Hepatobiliary Pancreat Sci. 2014 Aug;21(8):607-15. [Content Brief]

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