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PF-4989216

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Chemical Structure| 1276553-09-3 同义名 : -
CAS号 : 1276553-09-3
货号 : A607709
分子式 : C18H13FN6OS
纯度 : 99%+
分子量 : 380.399
MDL号 : MFCD28386245
存储条件：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(78.86 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • p110γ

    p110γ, IC50:65 nM

  • p110α

    p110α, IC50:2 nM

  • p110δ

    p110δ, IC50:1 nM
描述 PF-4989216 possesses outstanding PI3Kα Ki (0.6 nM), good cellular potency with S473 IC50 of 79 nM, and high selectivity against mTOR with mTOR Ki of 1440 nM. It exhibits excellent selectivity against over 40 other kinases, with minimal major CYP inhibitions. Inhibition levels of less than 30% are observed in 1A2, 2C9, 2D6, and 3A4 CYP enzymes at 3 μM [1]. The toxicity profile of PF-4989216 is evaluated across various drug-sensitive and multidrug-resistant (MDR) cancer cell lines, including those overexpressing ABCB1 or ABCG2, as well as in HEK293 cells transfected with human ABCB1 or ABCG2. PF-4989216 exhibits inhibitory effects on human colon carcinoma S1 cells and ABCG2-overexpressing subline S1-M1-80 with IC50 values of 1.11±0.09 and 6.79±1.00 μM, respectively. It also inhibits human breast carcinoma MCF-7 and ABCG2-overexpressing sublines MCF7-FLV1000 and MCF7-AdVp3000 with IC50 values of 2.30±0.68, 23.26±2.94, and 62.57±5.46 μM, respectively. Moreover, PF-4989216 inhibits pcDNA-HEK293, ABCB1-transfected MDR19-HEK293, and ABCG2-transfected R482-HEK293 cells with IC50 values of 0.44±0.05, 0.38±0.06, and 5.05±0.89 μM, respectively [2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.63mL

0.53mL

0.26mL

13.14mL

2.63mL

1.31mL

26.29mL

5.26mL

2.63mL