529584
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, VEGFR Tyrosine Kinase Inhibitor XXXII, VEGFR2 Kinase Inhibitor XXX
For general questions please contact our Customer Service:
EMD Millipore
290 Concord Road
01821 Billerica, MA
United States
Phone: 781 533-6000
Fax: +49 6151 72 2000
E-mail: Customer.CareDesk@emdchemicals.com
26 May 2012
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A cell-permeable pyrazolopyrimidine compound that effectively targets the ATP pocket of both protein tyrosine kinases (IC50 <0.26 µM against Abl, EGFR, EphB4, Hck, PDGFR, RET, Src, SrcT338I, and VEGFR2) and PI 3-K family kinases (IC50 <1.4 µM 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 µM inhibitor and 10 µM 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, Cat. Nos. 528100 and 528101) is shown to be less effective than PP121 treatment (IC50 = 50 nM) in inhibiting the proliferation of Ret C634W-expressing TT thyroid carcinoma cultures.
| Product information | |||
|---|---|---|---|
| Form | White solid | ||
| Molar mass | 319.4 | ||
| Protect from Light | Yes | ||
| Packaged under inert gas | Yes | ||
| Purity | ≥98% by HPLC | ||
| Solubility | DMSO | ||
| Chemical formula | C17H17N7 | ||
| CAS number | 1092788-83-4 | ||
| Store and ship information | |||
|---|---|---|---|
| Storage | -20°C | ||
| Ship |
Ambient Temperature Only
Standard Handling |
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