CAS NO: | 2682114-54-9 |
生物活性 | SP-96 is a highly potent, selective and non-ATP-competitiveAurora B(IC50=0.316 nM) inhibitor and shows >2000 fold selectivity againstFLT3and KIT. SP-96 shows selective growth inhibition in NCI60 screening, incluing MDA-MD-468 (GI50=107 nM). SP-96 can be used for the research of triple negative breastcancer(TNBC)[1]. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | SP-96 is a highly potent, selective and non-ATP-competitiveAurora B(IC50=0.316 nM) inhibitor and shows >2000 fold selectivity against FLT3 (IC50=1475.6 nM) and KIT (IC50=1307.6 nM)[1].SP-96 (0-1 μM; 24 hours) is not promiscuous, rather selective for a few cell lines, it inhibits MDA-MB-468, CCRF-CEM, COLO 205 and A498 cell growth with GI50values of 107 nM,47.4 nM, 50.3 nM and 53.2 nM, respectively[1].SP-96 (63.2 nM) inhibits Aurora B activity in H460 cells by the characteristics of increased DNA content, and it increases cell volume with enormous nucleus[1].SP-96 (0-2 μM) inhibits Aurora B enzymatic activity with an IC50of 0.316 nM and inhibits Aurora A with observed IC50value of 18.975 nM. SP-96 shows >2000 fold selectivity against FLT3 (IC50=1475.6 nM) and KIT (IC50=1307.6 nM). Meanwhile, it exhibits inhibitory effects on other receptor tyrosine kinases (RTKs) namely EGFR, RET and HER2 with IC50value ≥2 μM[1]. Cell Viability Assay[1]
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分子量 | 453.47 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C25H20FN7O | ||||||||||||||||
CAS 号 | 2682114-54-9 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 100 mg/mL(220.52 mM;Need ultrasonic) 配制储备液
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