SIAIS178
作者：齊岳
發布時間：2023-08-23
09:21:38
點擊數：
產品名稱：SIAIS178
產品描述：
| 產品描述 | SIAIS178 is a potent and selective degrader of BCR-ABL based on PROTAC technology (IC50 of 24 nM). |
| 靶點活性 | VHL:24 nM, Bcr-Abl:24 nM |
| 體外活性 | 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. |
| 體內活性 | 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 |
存儲
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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