SMI-16a

产品编号: DC10514 Featured
SMI-16a
结构式
587852-28-6
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中国地区超过5000个高品质化合物库存
应用领域
SMI-16a是选择性的 Pim 激酶抑制剂,对Pim1,Pim2 和 PC3 细胞的IC50值分别为0.15,0.02 和48 μM。
Cas No.: 587852-28-6
名称:
别名: SMI-16a,SMI 16a,SMI16a
SMILES: CCCOC1=CC=C(C=C1)/C=C\2/C(=O)NC(=O)S2
分子式: C13H13NO3S
分子量: 263.31
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: 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.SMI-16a has excellent potency for inhibition of both Pim-1 and Pim-2. 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.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. SMI-16a effectively prevents bone destruction while suppressing MM tumor growth in MM animal models.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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