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587852-28-6

中文名稱 PIM1/2 KINASE INHIBITOR VI
英文名稱 SMI-16a
CAS 587852-28-6
分子式 C13H13NO3S
分子量 263.31
MOL 文件 587852-28-6.mol
更新日期 2025/01/23 13:36:08
587852-28-6 結(jié)構(gòu)式 587852-28-6 結(jié)構(gòu)式

基本信息

中文別名
化合物SMI-16A
PIM激酶抑制劑(SMI-16A)
英文別名
SMI-16a
SMI-16A
SMI 16A
SMI16A
PIM1/2 Kinase Inhibitor VI
SMI-16a(PIM1/2 Kinase Inhibitor VI)
2,4-Thiazolidinedione, 5-[(4-propoxyphenyl)methylene]-

物理化學(xué)性質(zhì)

熔點(diǎn)186.3-188.4 °C
密度1.303±0.06 g/cm3(Predicted)
儲存條件Keep in dark place,Sealed in dry,2-8°C
溶解度Ethanol:3.0(Max Conc. mg/mL);11.39(Max Conc. mM)
酸度系數(shù)(pKa)7.27±0.20(Predicted)
形態(tài)A solid
顏色Light yellow to yellow

常見問題列表

生物活性
SMI-16a是選擇性Pim激酶抑制劑,對Pim1和Pim2的IC50值分別為150 nM和20 nM。
靶點(diǎn)
TargetValue
Pim2
()
20 nM
Pim1
()
150 nM
體外研究

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.

體內(nèi)研究

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.

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