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

616456
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Overview

Replacement Information

Key Specifications Table

Empirical FormulaCAS #
C₁₇H₁₀ClFN₆ 627536-09-8

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616456-2MG
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      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®
      SynonymsTransforming Growth Factor-β Type I Receptor Kinase Inhibitor V, 2-(5-Chloro-2-fluorophenyl)pteridin-4-yl)pyridin-4-yl amine, SD-208, 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

      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.
      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
      SynonymsTransforming Growth Factor-β Type I Receptor Kinase Inhibitor V, 2-(5-Chloro-2-fluorophenyl)pteridin-4-yl)pyridin-4-yl amine, SD-208, 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 +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 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.