SIAIS178

Name: SIAIS178
Brand: TargetMol
SKU: T12907
Rating: 4.5 (1 reviews)

还可以

产品编号 T12907Cas号 2376047-73-1

SIAIS178 is a potent and selective degrader of BCR-ABL based on PROTAC technology (IC50 of 24 nM).

为众多的药物研发团队赋能，

让新药发现更简单！

还可以

产品编号 T12907Cas号 2376047-73-1

SIAIS178 is a potent and selective degrader of BCR-ABL based on PROTAC technology (IC50 of 24 nM).

大包装 & 定制

加入购物车

TargetMol 的所有产品仅用作科学研究或药证申报，不能被用于人体，我们不向个人提供产品和服务。请您遵守承诺用途，不得违反法律法规规定用于任何其他用途。

实验操作小课堂

常见问题解答

联系我们获取更多批次信息

资源下载

产品介绍

生物活性

产品描述	SIAIS178 is a potent and selective degrader of BCR-ABL based on PROTAC technology (IC50 of 24 nM).
靶点活性	VHL:24 nM, BCR-ABL:24 nM
体外活性	the BCR-ABL protein levels in a concentration dependent manner significantly reduced by SIAIS178 (1-100 nM; for 16 hours) . SIAIS178 significantly inhibits the phosphorylation of BCR-ABL and the substrates STAT5. in BCR-ABL driven CML cell lines, SIAIS178 (1, 10, 100, 1000 nM) exerts significant antiproliferative activity. SIAIS178 retains potency and selectivity against the BCR-ABL driven cell lines.
体内活性	Tumor progression in a dose-dependent manner attenuated by SIAIS178 (ip; 5, 15, and 45 mg/kg; 12 days), as determined by serial volumetric measurement . SIAIS178 (iv or ip; 2 mg/kg; 24 hours) has T1/2 of 3.82 and 12.35 hours and Cmax of 1165.2 nM and 30 nM for iv and ip, respectively.

化学信息

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

DMSO: 300 mg/mL (296.24 mM), Sonication is recommended.

溶液配制表

DMSO