CAS NO: | 870281-82-6 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
生物活性 | Idelalisib (CAL-101; GS-1101) is a highly selective and orally bioavailablep110δinhibitor with anIC50of 2.5 nM, showing 40- to 300-fold selectivity for p110δ over otherPI3Kclass I enzymes. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | Idelalisib (CAL-101; GS-1101) is a highly selective and potent p110δ inhibitor (EC50=8 nM). Greater selectivity (400- to 4000-fold) is seen against related kinases C2β, hVPS34, DNA-PK, and mTOR, whereas no activity is observed against a panel of 402 diverse kinases at 10 μM. CAL-101 reduces PDGF-induced pAkt by only 25% at 10 μM. Idelalisib (CAL-101) inhibits LPA-induced pAkt with an EC50of 1.9 μM. Idelalisib (CAL-101) blocks FcεRI p110δ-mediated CD63 expression with an EC50of 8 nM, whereas formyl-methionyl-leucyl-phenylalanine activation of p110γ is inhibited with an EC50of 3 μM. Thus, in cell-based assays, CAL-101 has 240- to 2500-fold selectivity for p110δ over the other class I PI3K isoforms[1]. CAL-101Idelalisib (CAL-101)-induced apoptosis of chronic lymphocytic leukemia (CLL) cells is significant compare with vehicle treatment alone (P<0.001). Idelalisib (CAL-101) induces selective cytotoxicity in CLL cells independent of IgVH mutational status or interphase cytogenetics[2]. | ||||||||||||||||
体内研究 (In Vivo) | A significant reduction is observed in the CD11b+Ly6G+neutrophils from brain homogenates of bothp110δD910A/D910Amice and Idelalisib (CAL-101) (40 mg/kg, i.v.) post-treated mice[3]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 415.42 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C22H18FN7O | ||||||||||||||||
CAS 号 | 870281-82-6 | ||||||||||||||||
中文名称 | 艾代拉里斯;艾代拉利司;艾拉利司 | ||||||||||||||||
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 : ≥ 59.7 mg/mL(143.71 mM) *"≥" means soluble, but saturation unknown. 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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