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Merck
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Key Documents

529584

Sigma-Aldrich

PTK/PI 3-K/mTOR Inhibitor, PP121

The PTK/PI 3-K/mTOR Inhibitor, PP121, also referenced under CAS 1092788-83-4, controls the biological activity of PTK/PI 3-K/mTOR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

别名:

PTK/PI 3-K/mTOR Inhibitor, PP121, 1-Cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, PI 3-K/mTOR Inhibitor II, PDGFR Tyrosine Kinase Inhibitor XVIII, Abl Inhibitor IV, mTOR Inhibitor VII, VEGFR Tyrosine Kinase Inhibitor XXXII, VEGFR2 Kinase Inhibitor XXX, PI 3-K Inhibitor XIII

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About This Item

经验公式(希尔记法):
C17H17N7
分子量:
319.36
MDL號碼:
分類程式碼代碼:
12352200
NACRES:
NA.77

品質等級

化驗

≥98% (HPLC)

形狀

solid

製造商/商標名

Calbiochem®

儲存條件

OK to freeze
protect from light

顏色

white

溶解度

DMSO: 100 mg/mL

運輸包裝

ambient

儲存溫度

−20°C

InChI

1S/C17H17N7/c18-15-13-14(11-7-10-5-6-19-16(10)20-8-11)23-24(12-3-1-2-4-12)17(13)22-9-21-15/h5-9,12H,1-4H2,(H,19,20)(H2,18,21,22)

InChI 密鑰

NVRXTLZYXZNATH-UHFFFAOYSA-N

一般說明

A cell-permeable pyrazolopyrimidine compound that effectively targets the ATP pocket of both protein tyrosine kinases (IC50<0.26 M against Abl, EGFR, EphB4, Hck, PDGFR, RET, Src, SrcT338I, and VEGFR2) and PI 3-K family kinases (IC50<1.4 M against p110α/ β/ δ/ γ, mTOR, and DNA-PK). PP121 is less effective against ser/thr kinases and exhibits significant inhibition of only 14 ser/thr kinases (≥70% inhibition with 1 M inhibitor and 10 M ATP) in a 219 kinase panel screening. Individually targeting Ret by sorafenib (IC50 = 780 nM) or PI 3-K/mTOR pathway by PI-103 (IC50 = 800 nM) is shown to be less effective than PP121 treatment (IC50 = 50 nM) in inhibiting the proliferation of Ret C634W-expressing TT thyroid carcinoma cultures.

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重構

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他說明

Apsel, B., et al. 2008. Nat. Chem. Biol.4, 691.

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

儲存類別代碼

10 - Combustible liquids

水污染物質分類(WGK)

WGK 1

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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