化学性质:
规格 | 5mg 10mg 25mg 50mg 100mg 200mg |
CAS | 587852-28-6 |
别名 | N/A |
化学名 | N/A |
分子式 | C13H13NO3S |
分子量 | 263.31 |
溶解度 | DMSO: ≥ 100 mg/mL (379.78 mM) |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
SMI-16a is a selective Pim kinase inhibitor with IC50 values of 0.15, 0.02 and 48 μM for Pim1, Pim2 and PC3 cells, respectively. IC50: 0.15 μM (Pim1), 0.02 μM (Pim2), 48 μM (PC3 cells)[1]
SMI-16a has excellent potency for inhibition of both Pim-1 and Pim-2[1]. Treatment with Pim-2 short-interference RNA as well as the Pim inhibitor SMI-16a successfully restores osteoblastogenesis suppressed by all the above inhibitory factors and MM cells. The SMI-16a treatment potentiates BMP-2-mediated anabolic signaling while suppressing TGF-β signaling[2].
Mice tolerate intraperitoneal dose of SMI-16a is 50 mg/kg daily for 5 days, while 100 mg/kg is overtly toxic. Treatment of the animals with SMI-16a for 5 days per week reduces the growth of tumors by approximately 50% and does not cause a loss of body weight. Subchronic dosing with SMI-16a does not affect the levels of red, white blood cells, including lymphocytes, monocytes, and granulocytes, indicating that the compound does not have myelosuppressive effects. SMI-16a does not have toxicity toward the liver as the albumin, alkaline phosphatase, and alanine aminotransferase levels are unchanged [1]. SMI-16a effectively prevents bone destruction while suppressing MM tumor growth in MM animal models[2].
特别提醒:
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