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

A cell-permeable, highly potent, ATP-competitive multi-kinase inhibitor (IC₅₀ = 2, 3, 6, 8 nM for VEGFR1, VEGFR2, VEGFR3, and Kit, respectively).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: N-(3,3-dimethylindolin-6-yl)-2-((pyridin-4-ylmethyl)amino)nicotinamide, AMG-706

Primary Target: VEGFR
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538169
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
857876-30-3C₂₂H₂₃N₅O.2H₃PO₄

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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
      Quality LevelMQ100
      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
      Global Trade Item Number
      Catalogue Number GTIN
      5.38169.0001 04054839059414

      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 Protect from light
      -20°C
      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.
      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.