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616456 TGF-β RI Kinase Inhibitor V - CAS 627536-09-8 - Calbiochem

616456
  
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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
627536-09-8C₁₇H₁₀ClFN₆
Description
OverviewA cell-permeable pteridine compound that blocks TGF-β signaling and displays anti-tumor properties. Acts as a potent, selective, and reversible inhibitor of TGF-β RI/ALK5 kinase (EC50 = 48 nM). It inhibits p38α, MAPKAP, PKD, and p38α only at much higher concentrations (≥867 nM), while exhibiting little activity aginst TGF-β RII, p38γ, JNK, ERK2, MAPKK6, PKA, or PKC even at concentrations as high as 50 µM. Inhibits TGF-β-mediated cellular functions both in vitro and in vivo.
Catalogue Number616456
Brand Family Calbiochem®
Synonyms2-(5-Chloro-2-fluorophenyl)pteridin-4-yl)pyridin-4-yl amine, SD-208, Transforming Growth Factor-β Type I Receptor Kinase Inhibitor V, ALK5 Inhibitor V
References
ReferencesGe, R., et al. 2006. Clin. Cancer Res. 12, 4315.
Kapoun, A. M., et al. 2006. Mol. Pharmacol. 70, 518.
Jian, H., et al. 2006. Genes Dev. 20, 666.
Hayashi, T., et al. 2004. Clin. Cancer Res. 10, 7540.
Uhl, M., et al. 2004. Cancer Res. 64, 7954.
Product Information
CAS number627536-09-8
ATP CompetitiveN
FormLight yellow solid
Hill FormulaC₁₇H₁₀ClFN₆
Chemical formulaC₁₇H₁₀ClFN₆
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetTGF-β RI/ALK5 Kinase
Primary Target IC<sub>50</sub>EC50 = 48 nM against TGF-β RI/ALK5 kinase
Purity≥97% by 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 Regulatory Review
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
Global Trade Identification Number
Catalog Number GTIN
616456

Documentation

TGF-β RI Kinase Inhibitor V - CAS 627536-09-8 - Calbiochem Certificates of Analysis

TitleLot Number
616456

References

Reference overview
Ge, R., et al. 2006. Clin. Cancer Res. 12, 4315.
Kapoun, A. M., et al. 2006. Mol. Pharmacol. 70, 518.
Jian, H., et al. 2006. Genes Dev. 20, 666.
Hayashi, T., et al. 2004. Clin. Cancer Res. 10, 7540.
Uhl, M., et al. 2004. Cancer Res. 64, 7954.

Brochure

Title
TGF-b Signaling: Dual Role in Tumor Suppression and Oncogenesis
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.

Revision20-November-2008 JSW
Synonyms2-(5-Chloro-2-fluorophenyl)pteridin-4-yl)pyridin-4-yl amine, SD-208, Transforming Growth Factor-β Type I Receptor Kinase Inhibitor V, ALK5 Inhibitor V
DescriptionA cell-permeable pteridine compound that blocks TGF-β signaling and displays anti-tumor properties. Acts as a potent, selective, and reversible inhibitor of TGF-β RI/ALK5 kinase (EC50 = 48 nM). It inhibits p38α, MAPKAP, PKD, and p38α only at much higher concentrations (≥867 nM), while exhibiting little activity aginst TGF-β RII, p38γ, JNK, ERK2, MAPKK6, PKA, or PKC even at concentrations as high as 50 µM. Inhibits TGF-β-mediated cellular functions both in vitro and in vivo.
FormLight yellow solid
Intert gas (Yes/No) Packaged under inert gas
CAS number627536-09-8
Chemical formulaC₁₇H₁₀ClFN₆
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (5 mg/ml)
Storage Protect from light
+2°C to +8°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 Regulatory Review
ReferencesGe, R., et al. 2006. Clin. Cancer Res. 12, 4315.
Kapoun, A. M., et al. 2006. Mol. Pharmacol. 70, 518.
Jian, H., et al. 2006. Genes Dev. 20, 666.
Hayashi, T., et al. 2004. Clin. Cancer Res. 10, 7540.
Uhl, M., et al. 2004. Cancer Res. 64, 7954.