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328011 ERK Inhibitor VIII, VX-11e - CAS 896720-20-0 - Calbiochem

328011
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Replacement Information

Products

Número de referenciaEmbalaje Cant./Env.
328011-10MG Frasco de vidrio 10 mg
Description
OverviewA cell-permeable pyrimidylpyrrole compound that acts as an active site-targeting, highly potent and selective ERK1/2 inhibitor (KI <2 nM against Erk2; [ATP] = 65 µM), while inhibiting GSK-3, Aurora A, Cdk2 only at much higher concentrations (KI = 395, 540, and 852 nM, respectively) and exhibiting much reduced or little potency toward a panel of more than 130 other kinases (KI ≥1.4 µM; IC50 ≥1 µM). Shown to effectively inhibit human colon carcinoma HT-29 proliferation (IC50 = 48 nM) and restore EGFR inhibitor WZ4002 antiproliferation activity in WZR10 cultures (84% and no inhibition, respectively, by 100 nM WZ4002 with or without 1 µM Erk Inhibitor VIII co-treatment). Orally available in both mice and rats in vivo.
Catalogue Number328011
Brand Family Calbiochem®
SynonymsVX-11e, (S)-4-(2-(2-Chloro-4-fluorophenylamino)-5-methylpyrimidin-4-yl)-N-(1-(3-chlorophenyl)-2-hydroxyethyl)-1H-pyrrole-2-carboxamide
References
ReferencesErcan, D., et al. 2012. Cancer Discovery 2, 934.
Aronov, A.M., et al. 2009. J. Med. Chem. 52, 6362.
Product Information
CAS number896720-20-0
FormYellowish-white powder
Hill FormulaC₂₄H₂₀Cl₂FN₅O₂
Chemical formulaC₂₄H₂₀Cl₂FN₅O₂
ReversibleY
Structure formula ImageStructure formula Image
Applications
Biological Information
Primary TargetERK
Purity≥98% by Chiral HPLC
Physicochemical Information
Cell permeableY
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 +2°C to +8°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

Documentation

ERK Inhibitor VIII, VX-11e - CAS 896720-20-0 - Calbiochem Certificados de análisis

CargoNúmero de lote
328011

Referencias bibliográficas

Visión general referencias
Ercan, D., et al. 2012. Cancer Discovery 2, 934.
Aronov, A.M., et al. 2009. J. Med. Chem. 52, 6362.
Ficha técnica

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.

Revision10-May-2013 JSW
SynonymsVX-11e, (S)-4-(2-(2-Chloro-4-fluorophenylamino)-5-methylpyrimidin-4-yl)-N-(1-(3-chlorophenyl)-2-hydroxyethyl)-1H-pyrrole-2-carboxamide
DescriptionA cell-permeable pyrimidylpyrrole compound that acts as an active site-targeting, highly potent and selective ERK1/2 inhibitor (KI <2 nM against Erk2; [ATP] = 65 µM), while inhibiting GSK-3, Aurora A, Cdk2 only at much higher concentrations (KI = 395, 540, and 852 nM, respectively) and exhibiting much reduced or little potency toward a panel of more than 130 other kinases (KI ≥1.4 µM; IC50 ≥1 µM). Shown to effectively inhibit human colon carcinoma HT-29 proliferation (IC50 = 48 nM) and be orally available in both mice (F = 67%; t1/2 = 4.4 h; Plasma conc. = 488 and 122 ng/mL, respectively, 4 h and 8 h post single 33 mg/kg oral dosage) and rats (F = 65%; t1/2 = 3 h; Plasma conc. = 329 and 267 ng/mL, respectively, 4 h and 8 h post single 10 mg/kg oral dosage) in vivo. Also reported to restore EGFR inhibitor WZ4002 antiproliferation activity in WZR10 cultures (84% and no inhibition, respectively, by 100 nM WZ4002 with or without 1 µM Erk Inhibitor VIII co-treatment).
FormYellowish-white powder
Intert gas (Yes/No) Packaged under inert gas
CAS number896720-20-0
Chemical formulaC₂₄H₂₀Cl₂FN₅O₂
Structure formulaStructure formula
Purity≥98% by Chiral HPLC
SolubilityDMSO (50 mg/ml)
Storage +2°C to +8°C
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.
Toxicity Standard Handling
ReferencesErcan, D., et al. 2012. Cancer Discovery 2, 934.
Aronov, A.M., et al. 2009. J. Med. Chem. 52, 6362.