Chemdea |
pp121 – Tyrosin Kinase and PI3K Pathway Inhibitor |
Catalog # CD0257 |
Price: 1 mg - $35;
5 mg - $55; 10 mg - $75; 25 mg - $130; 50 mg - $220; 100 mg - $395; 200 mg -
$750 |
Availability: In stock |
1-Cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1Hpyrazolo[3,4-d]pyrimidin-4-amine
White solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. Purity: 99% by HPLC. CAS# 1092788-83-4. Solubility: DMSO (100 mg/mL), ethanol (50 mg/mL). Molecular Formula: C17H17N7. Molecular Weight: 319.4.
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, Src, and VEGFR2) and PI3-K T338I 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 mM ATP) in a 219 kinase panel screening. Individually targeting Ret by sorafenib (IC50 = 780 nM) or PI3-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. Reference: Apsel, B. et al. Nat. Chem. Biol. 2008, 4, 691. |
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Cat. No. 529584 |
Cat. No. 3894 |
Cat. No. P036 |
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