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444967 MEK1/2 Inhibitor IV - CAS 212631-67-9 - Calbiochem

444967
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
212631-67-9C₁₇H₁₃BrClF₂IN₂O₂

Products

Catalogue NumberPackaging Qty/Pack
444967-5MG 5 mg
Description
OverviewA cell-permeable, blood-brain barrier permeant, and orally active hydroxamate compound that is reported to inhibit MEK activity (IC50 = 10-100 nM) without competing against ATP or Erk binding and exhibit excellent selectivity over 27 other cellular kinases, including JNK, MAPK2/ERK2, SAPK2a, SAPK2b, SAPK3, and SAPK4 (IC50 > 10 µM). Shown to be superior to PD 98059 (Cat. Nos. 513000 and 513001) and U0126 (Cat. No. 662005) in suppressing Erk1/2 phosphorylation in Hep3B, HepG2, PLC, and SKHep human liver cancer cells (IC50 <0.1 µM) in vitro and effectively reduce Erk1/2 phosphorylation in hippocampal tissue in mice (ED50 <50 mg/kg, i.p.) in vivo. Both PD184161 and U0126 are shown to induce necrosis of several types of glucose-deprived cells via an indirect action on the F0 component of the mitochondrial F1F0-ATPase/synthase.
Catalogue Number444967
Brand Family Calbiochem®
Synonyms2-(2-Chloro-4-iodo-phenylamino)-N-cyclopropylmethoxy-3,4-difluoro-5-bromo-benzamide, PD184161, MEK Inhibitor IV
References
ReferencesYip-Schneider, M.T., et al. 2009. J. Pharmacol. Exp. Ther. 329, 1063.
Duman, C.H., et al. 2007. Biol. Psychiatry 61, 661.
Klein, P.J., et al. 2006. Neoplasia 8, 1.
Thottassery, J.V., et al. 2004. Cancer Res. 64, 4637.
Yung, H.W., et al. 2004. Biochem. Pharmacol. 68, 351.
Product Information
CAS number212631-67-9
FormWhite solid
Hill FormulaC₁₇H₁₃BrClF₂IN₂O₂
Chemical formulaC₁₇H₁₃BrClF₂IN₂O₂
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 +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 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

MEK1/2 Inhibitor IV - CAS 212631-67-9 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

MEK1/2 Inhibitor IV - CAS 212631-67-9 - Calbiochem Certificates of Analysis

TitleLot Number
444967

References

Reference overview
Yip-Schneider, M.T., et al. 2009. J. Pharmacol. Exp. Ther. 329, 1063.
Duman, C.H., et al. 2007. Biol. Psychiatry 61, 661.
Klein, P.J., et al. 2006. Neoplasia 8, 1.
Thottassery, J.V., et al. 2004. Cancer Res. 64, 4637.
Yung, H.W., et al. 2004. Biochem. Pharmacol. 68, 351.
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.

Revision15-July-2010 RFH
Synonyms2-(2-Chloro-4-iodo-phenylamino)-N-cyclopropylmethoxy-3,4-difluoro-5-bromo-benzamide, PD184161, MEK Inhibitor IV
DescriptionA cell-permeable, blood-brain barrier permeant, and orally active hydroxamate compound that is reported to inhibit MEK activity (IC50 = 10-100 nM) without competing against ATP or Erk binding and exhibit excellent selectivity over 27 other cellular kinases, including JNK, MAPK2/ERK2, SAPK2a, SAPK2b, SAPK3, and SAPK4 (IC50 > 10 µM). Shown to be superior to PD 98059 (Cat. Nos. 513000 and 513001 and U0126 (Cat. No. 662005) in suppressing Erk1/2 phosphorylation in Hep3B, HepG2, PLC, and SKHep human liver cancer cells (IC50 <0.1 µM) in vitro and effectively reduce Erk1/2 phosphorylation in hippocampal tissue in mice (ED50 <50 mg/kg, i.p.) in vivo. Both PD184161 and U0126 are shown to induce necrosis of several types of glucose-deprived cells via an indirect action on the F0 component of the mitochondrial F1F0-ATPase/synthase.
FormWhite solid
Intert gas (Yes/No) Packaged under inert gas
CAS number212631-67-9
Chemical formulaC₁₇H₁₃BrClF₂IN₂O₂
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (100 mg/ml) or Ethanol (5 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 3 months at -20°C.
Toxicity Standard Handling
ReferencesYip-Schneider, M.T., et al. 2009. J. Pharmacol. Exp. Ther. 329, 1063.
Duman, C.H., et al. 2007. Biol. Psychiatry 61, 661.
Klein, P.J., et al. 2006. Neoplasia 8, 1.
Thottassery, J.V., et al. 2004. Cancer Res. 64, 4637.
Yung, H.W., et al. 2004. Biochem. Pharmacol. 68, 351.