526528
PIM-Kinase Inhibitor IX, SGI-1776
The PIM-Kinase Inhibitor IX, SGI-1776 controls the biological activity of PIM-Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
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所有图片(2)
PIM-Kinase Inhibitor IX, SGI-1776, N-((1-Methylpiperidin-4-yl)methyl)-3-(3-(trifluoromethoxy)phenyl)imidazo[1,2-b]pyridazin-6-amine, 2H₂SO₄
C20H22F3N5O · 2H2SO4
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质量水平
检测方案
≥99% (HPLC)
形式
powder
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
desiccated (hygroscopic)
protect from light
颜色
off-white
溶解性
DMSO: 100 mg/mL, clear, nearly colorless
water: 100 mg/mL, clear, nearly colorless
运输
ambient
储存温度
2-8°C
SMILES字符串
CN(CC1)CCC1CNC(C=C2)=NN3C2=NC=C3C4=CC(OC(F)(F)F)=CC=C4
一般描述
A cell-permeable imidazopyridazine compound that acts as a potent, reversible and ATP-competitive inhibitor of Pim-1,2,3, Flt-3 and haspin kinase activities (IC50 = 7, 363, 69, 44 and 34 nM, respectively) with moderate (40% inhibition at 1 µM for c-kit) to excellent selectivity over CDKs, Aurora, Chk1, IKK, JNK, Abl, Raf, PKA, PKC and PI 3-K among 300-kinases. Shown to inhibit RNA synthesis, block phosphorylation of c-Myc-Ser62 and STAT3-Tyr705, and decrease c-Myc and Mcl-1 protein levels; cause cell cycle arrest and induce apoptosis in CLL lymphocytes and in AML cells, and efficiently arrest the growth of several prostate cancer cells (IC50<10 µM).
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重悬
Following reconstituion, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
其他说明
Chen, L.S., et al. 2011. Blood118, 693.
Chang, M., et al. 2010. Mol. Cancer Ther.9, 2478.
Mumenthaler, S.M., et al. 2009. Mol. Cancer Ther.8, 2882.
Chen, L.S., et al. 2009. Blood 114, 4150.
Chang, M., et al. 2010. Mol. Cancer Ther.9, 2478.
Mumenthaler, S.M., et al. 2009. Mol. Cancer Ther.8, 2882.
Chen, L.S., et al. 2009. Blood 114, 4150.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 2
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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