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.

• Synonym(e): 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
• Empirische Formel (Hill-System): C₁₇H₁₇N₇
• CAS-Nummer: 1092788-83-4
• Molekulargewicht: 319.36
• MDL-Nummer: MFCD12912434
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥98% (HPLC)
• Form: solid
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: white
• Löslichkeit: DMSO: 100 mg/mL
• Versandbedingung: ambient
• Lagertemp.: −20°C
• SMILES String: [n]2(nc(c5c2ncnc5N)c3cnc4[nH]ccc4c3)C1CCCC1
• 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)
• InChIKey: NVRXTLZYXZNATH-UHFFFAOYSA-N

Beschreibung

Allgemeine Beschreibung

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.

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

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

Sonstige Hinweise

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

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 10 - Combustible liquids
• WGK: WGK 1
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable