529584

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.

• Synonim(y): 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
• Wzór empiryczny (zapis Hilla): C₁₇H₁₇N₇
• Numer CAS: 1092788-83-4
• Masa cząsteczkowa: 319.36
• Numer MDL: MFCD12912434
• Kod UNSPSC: 12352200
• NACRES: NA.77

Właściwości

• Poziom jakości: 100
• Próba: ≥98% (HPLC)
• Postać: solid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: white
• rozpuszczalność: DMSO: 100 mg/mL
• Warunki transportu: ambient
• temp. przechowywania: −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)
• Klucz InChI: NVRXTLZYXZNATH-UHFFFAOYSA-N

Opis

Opis ogólny

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, Src^T338I, 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.

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Rekonstytucja

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

Inne uwagi

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

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 10 - Combustible liquids
• Klasa zagrożenia wodnego (WGK): WGK 1
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable