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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
538169
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Přehled

Replacement Information

Tabulka spec. kláve

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

Products

Katalogové čísloBalení ks/bal.
5.38169.0001 Skleněná láhev 10 mg
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
Katalogové číslo GTIN
5.38169.0001 04054839059414

Documentation

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

Title

Safety Data Sheet (SDS) 

References

Přehled odkazů
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.