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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

      Empirical FormulaCAS #
      C₁₇H₁₀ClFN₆ 627536-09-8

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      616456-2MG
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          Plastic Bag(s) 2 mg
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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 Image
          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

          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
          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 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.