CAS NO: | 915019-65-7 |
包装 | 价格(元) |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
1 g | 电议 |
5 g | 电议 |
生物活性 | Dactolisib (BEZ235) is an orally active and dual pan-class IPI3KandmTORkinase inhibitor withIC50s of 4 nM/5 nM/7 nM/75 nM, and 20.7 nM forp110α/p110γ/p110δ/p110βandmTOR, respectively. Dactolisib (BEZ235) inhibits bothmTORC1andmTORC2. | ||||||||||||||||
IC50& Target |
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体外研究 (In Vitro) | Dactolisib (BEZ235) potently inhibits PI3K in an ATP Competitive Manner. Dactolisib (BEZ235) (250 nM) significantly reduced the phosphorylation levels of the mTOR activated kinase p70S6K. Dactolisib (BEZ235) also leads to a reduction of S235/S236P-RPS6 levels with an IC50of 6.5 nM, suggesting that Dactolisib (BEZ235) can directly inhibit the mTOR kinase, as the kinase domain of mTOR is highly homologous to the one of class IA PI3K. The activity of Dactolisib (BEZ235) against mTOR is confirmed using a biochemical mTOR K-LISA assay (IC50, 20.7 nM)[1]. The IC50s of Dactolisib (BEZ235) for HCT116, DLD-1, and SW480 cell lines are 14.3±6.4, 9.0±1.5, and 12.0±1.6 nM, respectively[2]. | ||||||||||||||||
体内研究 (In Vivo) | Dactolisib (BEZ235) (45 mg/kg, p.o.) treatment induces colonic tumor regression in a GEM model for sporadic PIK3CA wild-type CRC[2]. Dactolisib (BEZ235) (45 mg/kg) is administered to MENX rats (n=2 each group) by oral gavage and animals are sacrificed 1 or 6 hours after treatment. Immunostains for P-AKT and P-S6 show considerable reduction of the two proteins, and particularly of P-S6, 6 hours after administration of Dactolisib (BEZ235) when compares with PEG-treated rats. At 6 hours after treatment, the pituitary adenomas of Dactolisib (BEZ235)-treated rats has a proteomic profile significantly different from the tumors of placebo-treated rats[3]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 469.54 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C30H23N5O | ||||||||||||||||
CAS 号 | 915019-65-7 | ||||||||||||||||
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: 5% TFA : 8.33 mg/mL(17.74 mM;ultrasonic and warming and heat to 60℃) DMSO : 5 mg/mL(10.65 mM;ultrasonic and warming and heat to 60℃) DMF : 2 mg/mL(4.26 mM;Need ultrasonic) 配制储备液
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以下溶剂前显示的百
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