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529584 PTK/PI 3-K/mTOR Inhibitor, PP121 - CAS 1092788-83-4 - Calbiochem

529584
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1092788-83-4C₁₇H₁₇N₇

Products

Catalogue NumberPackaging Qty/Pack
529584-5MG 5 mg
Description
OverviewA 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.
Catalogue Number529584
Brand Family Calbiochem®
Synonyms1-Cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, PI 3-K/mTOR Inhibitor II, mTOR Inhibitor VII, Abl Inhibitor IV, PI 3-K Inhibitor XIII, VEGFR Tyrosine Kinase Inhibitor XXXII, VEGFR2 Kinase Inhibitor XXX, PDGFR Tyrosine Kinase Inhibitor XVIII
References
ReferencesApsel, B., et al. 2008. Nat. Chem. Biol. 4, 691.
Product Information
CAS number1092788-83-4
FormWhite solid
Hill FormulaC₁₇H₁₇N₇
Chemical formulaC₁₇H₁₇N₇
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥98% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
529584-5MG 04055977269901

Documentation

PTK/PI 3-K/mTOR Inhibitor, PP121 - CAS 1092788-83-4 - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

PTK/PI 3-K/mTOR Inhibitor, PP121 - CAS 1092788-83-4 - Calbiochem Certificates of Analysis

TitleLot Number
529584

References

Reference overview
Apsel, B., et al. 2008. Nat. Chem. Biol. 4, 691.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision25-May-2011 RFH
Synonyms1-Cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, PI 3-K/mTOR Inhibitor II, mTOR Inhibitor VII, Abl Inhibitor IV, PI 3-K Inhibitor XIII, VEGFR Tyrosine Kinase Inhibitor XXXII, VEGFR2 Kinase Inhibitor XXX, PDGFR Tyrosine Kinase Inhibitor XVIII
DescriptionA 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.
FormWhite solid
Intert gas (Yes/No) Packaged under inert gas
CAS number1092788-83-4
Chemical formulaC₁₇H₁₇N₇
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (100 mg/ml)
Storage Protect from light
-20°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesApsel, B., et al. 2008. Nat. Chem. Biol. 4, 691.