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538776 FGFR4 Inhibitor, BLU9931 - Calbiochem

Overview

Replacement Information

Key Spec Table

Empirical Formula
C₂₆H₂₂Cl₂N₄O₃

Products

Catalogue NumberPackaging Qty/Pack
5.38776.0001 Glass bottle 10 mg
Description
OverviewA cell-permeable anilinoquinazoline derivative that acts as a highly potent, irreversible, paralog selective inhibitor of fibroblast growth factor receptor 4 kinase (FGFR4; IC50 = 3 nM; kinact/KI = 0.6 x 105 (mol/L) -1s-1). Acts by forming a covalent bond with Cys552 within the ATP-binding pocket of FGFR4. Has minimal effect on FGFR1, 2, and 3 (IC50 = 591 nM, 493 nM, and 150 nM respectively) and does not display any activity towards a panel of 455 other protein kinases. Suppresses FGFR4 signaling and phosphorylation of downstream components in MDA-MB-453 cells. Also shown to be a potent inhibitor of downstream signaling in Hep 3B hepatocellular carcinoma (HCC) cells expressing FGF19 and induces caspase 3 and 7 activity. Inhibits the growth of Hep 3B HCC xenografts in murine model (100 mg/kg, b.i.d; p.o. for 21 days). Displays desirable pharmacokinetic properties with moderate bioavailability (18%) and t1/2 = 2.3 h (~ 10 mg/kg, p.o.).
Catalogue Number538776
Brand Family Calbiochem®
SynonymsFibroblast Growth Factor Receptor 4 Inhibitor, BLU9931
References
ReferencesHagel, M., et al. 2015. Cancer Discov. 5, 424.
Product Information
FormOff-white solid
Hill FormulaC₂₆H₂₂Cl₂N₄O₃
Chemical formulaC₂₆H₂₂Cl₂N₄O₃
ReversibleN
Quality LevelMQ100
Applications
Biological Information
Primary TargetFGFR4
Primary Target IC<sub>50</sub>3 nM
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
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
5.38776.0001 04054839119750

Documentation

FGFR4 Inhibitor, BLU9931 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Hagel, M., et al. 2015. Cancer Discov. 5, 424.
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.

Revision28-July-2017 JSW
SynonymsFibroblast Growth Factor Receptor 4 Inhibitor, BLU9931
DescriptionA cell-permeable anilinoquinazoline derivative that acts as a highly potent, irreversible, paralog selective inhibitor of fibroblast growth factor receptor 4 kinase (FGFR4; IC50 = 3 nM; kinact/KI = 0.6 x 105 (mol/L) -1s-1). Acts by forming a covalent bond with Cys552 within the ATP-binding pocket of FGFR4. Has minimal effect on FGFR1, 2, and 3 (IC50 = 591 nM, 493 nM, and 150 nM respectively) and does not display any activity towards a panel of 455 other protein kinases. Suppresses FGFR4 signaling and phosphorylation of downstream components in MDA-MB-453 cells. Also shown to be a potent inhibitor of downstream signaling in Hep 3B hepatocellular carcinoma (HCC) cells expressing FGF19 and induces caspase 3 and 7 activity. Inhibits the growth of Hep 3B HCC xenografts in murine model (100 mg/kg, b.i.d; p.o. for 21 days). Displays desirable pharmacokinetic properties with moderate bioavailability (18%) and t1/2 = 2.3 h (~ 10 mg/kg, p.o.).
FormOff-white solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₂₆H₂₂Cl₂N₄O₃
Purity≥98% by HPLC
SolubilityDMSO (100 mg/ml)
Storage Protect from light
-20°C
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
ReferencesHagel, M., et al. 2015. Cancer Discov. 5, 424.