Home > PI3K & > PF-04691502

PF-04691502

PF-04691502是ATP竞争性PI3K(α/β/δ/γ)和mTOR抑制剂，Ki分别为1.8 nM/2.1 nM/1.6 nM/1.9 nM和16 nM，对Vps34，AKT，PDK1，p70S6K，MEK，ERK，p38和JNK几乎无活性。

具体折扣请咨询客服

生物活性

PF-04691502 is a potent and selective, ATP-competitive PI3K/mTOR inhibitor with IC50 of 7.5 nM and 3.8 nM of AKT T308 and AKT S473, respectively. PF-04691502 is an ATP-competitive inhibitor which potently inhibits recombinant class I PI3K and FRAP and suppresses transformation of avian fibroblasts mediated by wild type PI3Kγ, δ or mutant PI3Kα. PF-04691502 has potential antineoplastic activity. PF-04691502 decreases phosphorylation of Akt T308 and Akt S473 in PIK3CA-mutant and PTEN-deleted cancer cell lines, and inhibits cell proliferation with (IC50 = 179 to 313 nM).
体外研究
体内研究
激酶实验
细胞实验

0-3 mM
动物实验

每天 7.5 或 10 mg/kg 口服喂食
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数

例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

参考文献

[1] Yuan et al (2011) PF-04691502, a potent and selective oral inhibitor of PI3K and mTOR kinases with antitumor activity. Mol.Cancer Ther. 10 2189.

分子式 C22H27N5O4	分子量 425.48	CAS号 1013101-36-4	储存方式 ﹣20 ℃冷藏长期储存。冰袋运输
溶剂（常温）	DMSO 14 mg/mL	Water <1 mg/mL	Ethanol <1 mg/mL

体内溶解度

NCT Number	Conditions	Interventions	Sponsor/Collaborators	Phases	Start Date	Last Updated
NCT00927823	Cancer	Drug: PF-04691502	Pfizer	Phase 1	2009-12-01	2014-07-18
NCT01658176	Breast Neoplasms	Drug: PF-04691502\|Drug: Exemestane\|Drug: Exemestane	Pfizer	Phase 2	2013-01-01	2012-10-26
NCT01430585	Early Breast Cancer (Phase 2)\|Advanced Breast Cancer (Phase 1b)	Drug: PF-04691502\|Drug: PF-04691502 in combination with Letrozole\|Drug: Letrozole	Pfizer	Phase 2	2012-03-01	2014-07-18
NCT01420081	Endometrial Neoplasms	Drug: PF-05212384\|Drug: PF-05212384\|Drug: PF-05212384	Pfizer	Phase 2	2012-01-01	2016-05-25
NCT01347866	Advanced Cancer	Drug: PF-05212384\|Drug: PD-0325901\|Drug: PF-05212384\|Drug: irinotecan	Pfizer	Phase 1	2011-10-01	2016-01-13

注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。