SIAIS178
作者：齐岳
发布时间：2023-08-23
09:21:38
点击数：
产品名称：SIAIS178
产品描述：
| 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. |
| 分子量 | 1012.68 |
| 分子式 | C50H62ClN11O6S2 |
| CAS No. | 2376047-73-1 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 300 mg/mL (296.24 mM),Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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