538169 Motesanib, Diphosphate - CAS 857876-30-3 - Calbiochem

538169
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₂H₂₃N₅O.2H₃PO₄ 857876-30-3

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      5.38169.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable, bioavailable nicotinamide derivative that acts as a highly potent, ATP-competitive multi-kinase inhibitor (IC50 = 2, 3, 6, 8 nM for VEGFR1, VEGFR2, VEGFR3, and Kit, respectively). Also inhibits the activity of PDGFR and RET kinases, albeit at higher concentrations (IC50 = 84 and 39 nM, respectively). Does not affect the activities of EGFR, Src, and p38 kinases (IC50 > 3 µM) and 47 other protein kinases. Inhibits VEGF-induced (IC50 = 10 nM), but not bFGF-induced (IC50 > 3 µM) proliferation of HUVECs. Also shown to diminish VEGF-induced angiogenesis in a rat corneal model (ED50 = 2.1 mg/kg, b.i.d; p.o.) and suppresses the growth of A431 human epidermoid xenografts in mice (10 to 100 mg/kg, b.i.d). Displays desirable pharmacokinetic properties (t = 6.7 h; Cmax = 787 ng/ml).

          Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
          Catalogue Number538169
          Brand Family Calbiochem®
          SynonymsN-(3,3-dimethylindolin-6-yl)-2-((pyridin-4-ylmethyl)amino)nicotinamide, AMG-706
          DescriptionMotesanib, Diphosphate
          References
          ReferencesWang, Y., et al. 2014. Biochem. Pharmacol. 90, 367.
          Benjamin, R., et al. 2011. Cancer Chemother. Pharmacol. 68, 69.
          Li, C., et al. 2009. Drug Metab. Dispos. 37, 1378.
          Sherman, S., et al. 2008. N. Engl. J. Med. 359, 31.
          Polverino, A., et al. 2006. Cancer Res. 66, 8715.
          Product Information
          CAS number857876-30-3
          FormOff-white solid
          Hill FormulaC₂₂H₂₃N₅O.2H₃PO₄
          Chemical formulaC₂₂H₂₃N₅O.2H₃PO₄
          Hygroscopic Hygroscopic
          ReversibleY
          Applications
          Biological Information
          Primary TargetVEGFR
          Primary Target IC<sub>50</sub>2 nM, 3 nM, 6 nM, 6 nM, 8 nM for VEGFR1, VEGFR2, Flk-1, VEGFR3, and KIT respecitively
          Purity≥98% 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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
          Toxicity Standard Handling
          Storage -20°C
          Protect from Light Protect from light
          Hygroscopic Hygroscopic
          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

          Motesanib, Diphosphate - CAS 857876-30-3 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Wang, Y., et al. 2014. Biochem. Pharmacol. 90, 367.
          Benjamin, R., et al. 2011. Cancer Chemother. Pharmacol. 68, 69.
          Li, C., et al. 2009. Drug Metab. Dispos. 37, 1378.
          Sherman, S., et al. 2008. N. Engl. J. Med. 359, 31.
          Polverino, A., et al. 2006. Cancer Res. 66, 8715.
          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.

          Revision09-September-2016 JSW
          SynonymsN-(3,3-dimethylindolin-6-yl)-2-((pyridin-4-ylmethyl)amino)nicotinamide, AMG-706
          DescriptionA cell-permeable, bioavailable nicotinamide derivative that acts as a highly potent, ATP-competitive multi-kinase inhibitor (IC50 = 2, 3, 6, 8 nM for VEGFR1, VEGFR2, VEGFR3, and Kit, respectively). Also inhibits the activity of PDGFR and RET kinases, albeit at higher concentrations (IC50 = 84 and 39 nM, respectively). Does not affect the activities of EGFR, Src, and p38 kinases (IC50 > 3 µM) and 47 other protein kinases. Inhibits VEGF-induced (IC50 = 10 nM), but not bFGF-induced (IC50 > 3 µM) proliferation of HUVECs. Also shown to diminish VEGF-induced angiogenesis in a rat corneal model (ED50 = 2.1 mg/kg, b.i.d; p.o.) and suppresses the growth of A431 human epidermoid xenografts in mice (10 to 100 mg/kg, b.i.d). Displays desirable pharmacokinetic properties (t = 6.7 h; Cmax = 787 ng/ml).
          FormOff-white solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number857876-30-3
          Chemical formulaC₂₂H₂₃N₅O.2H₃PO₄
          Purity≥98% by HPLC
          SolubilityDMSO (50 mg/ml)
          Storage -20°C
          Hygroscopic
          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
          ReferencesWang, Y., et al. 2014. Biochem. Pharmacol. 90, 367.
          Benjamin, R., et al. 2011. Cancer Chemother. Pharmacol. 68, 69.
          Li, C., et al. 2009. Drug Metab. Dispos. 37, 1378.
          Sherman, S., et al. 2008. N. Engl. J. Med. 359, 31.
          Polverino, A., et al. 2006. Cancer Res. 66, 8715.