Gedatolisib (PF-05212384, PKI-587)

Chemical Structure : Gedatolisib

CAS No.: 1197160-78-3

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货号: PC-60057Not For Human Use, Lab Use Only.

Gedatolisib (PF-05212384, PKI-587) is a highly potent, selective, dual PI3K/mTOR inhibitor with IC50 of 0.4/6/8/6/1.6 nM for PI3Kα/β/γ/δ/mTOR, respectively.

规格	价格	库存
10 mg	￥780	In stock
25 mg	￥1280	In stock
50 mg	￥2180	In stock
100 mg	￥3580	In stock
250 mg		Get quote

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生物&药学活性

Gedatolisib (PF-05212384, PKI-587) is a highly potent, selective, dual PI3K/mTOR inhibitor with IC50 of 0.4/6/8/6/1.6 nM for PI3Kα/β/γ/δ/mTOR, respectively.
PF-05212384 also potently inhibits PI3Kα mutant H1047R and E545K with IC50 of 0.6 and 0.6 nM.
PF-05212384 prevents the pAkt at Thr 308 with IC50 of 8 nM, and suppresses pAkt S473 with IC50 of <10 nM in cells.
PF-05212384 demonstrates antitumor efficacy in both subcutaneous and orthotopic xenograft tumor models.

物理化学性质&存储条件

分子量	615.72
分子式	C32H41N9O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	1-(4-{[4-(Dimethylamino)-1-piperidinyl]carbonyl}phenyl)-3-{4-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]phenyl}urea

参考文献

1. Venkatesan AM, et al. J Med Chem. 2010 Mar 25;53(6):2636-45.

2. Mallon R, et al. Clin Cancer Res. 2011 May 15;17(10):3193-203.

3. Gedaly R, et al. J Surg Res. 2013 Nov;185(1):225-30.

4. D'Amato V, et al. Br J Cancer. 2014 Jun 10;110(12):2887-95.