SIAIS178

Name: SIAIS178
Brand: TargetMol
SKU: T12907
Price: 633 USD
Availability: InStock
Rating: 4.5 (1 reviews)

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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).

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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).

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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