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505146 FMS/KIT Dual Kinase Inhibitor, PLX647 - Calbiochem

FMS/KIT Dual Kinase Inhibitor, PLX647 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: CDC2L6/CDK11/CDK19 Inhibitor, CDK8 Inhibitor, cFMS Inhibitor V, CSF-1 Receptor Inhibitor V, CSF1R Inhibitor V, DDR2 Inhibitor II, Flt-3 Inhibitor VIII, IL-34 Receptor Inhibitor V, NTRK3/TrkC Inhibitor, VEGFR Tyrosine Kinase Inhibitor XXXVI, VEGFR2 Tyrosine Kinase Inhibitor XXXIV, c-Kit Inhibitor IV, PLX-647

Primary Target: FMS
505146
  
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Áttekintés

Replacement Information

Kulcsspecifikációk táblázata

Empirical Formula
C₂₁H₁₇F₃N₄
Description
Overview

This product has been discontinued.



A cell-permeable and bio-available azaindolylmethylpyridamine derivative that acts as a potent inhibitor against FMS and KIT (IC50 = 28 and 16 nM, respectively) by targeting the kinases in their inactive DGF-out conformation, while being less effective against Flt3, KDR/VEGFR2, CDC2L6/CDK11/CDK19, NTRK3/TrkC, DDR2, CDK8/cyclin C (IC50 = 91, 130, 350, 620, 700, and 710 nM, respectively) and exhibiting much reduced or little potency toward other kinases in a 400-kinase panel study (IC50 >1 µM). Shown to effectively inhibit cellular FLT3-ITD, FMS, KIT phosphorylations (IC50 from 20 to 250 nM), as well as FLT3-ITD-, FMS-, KIT-dependent proliferations (IC50 from 92 to 380 nM). Exhibits in vivo efficacy in several murine inflammation models (20 to 80 mg/kg b.i.d.; p.o.) and in preventing rat MRMT-1 breast carcinoma bone metastases-caused osteolysis (30 mg/kg b.i.d.; p.o.).
Catalogue Number505146
Brand Family Calbiochem®
SynonymsCDC2L6/CDK11/CDK19 Inhibitor, CDK8 Inhibitor, cFMS Inhibitor V, CSF-1 Receptor Inhibitor V, CSF1R Inhibitor V, DDR2 Inhibitor II, Flt-3 Inhibitor VIII, IL-34 Receptor Inhibitor V, NTRK3/TrkC Inhibitor, VEGFR Tyrosine Kinase Inhibitor XXXVI, VEGFR2 Tyrosine Kinase Inhibitor XXXIV, c-Kit Inhibitor IV, PLX-647
References
ReferencesZhang, C., et al. 2013. Proc. Natl. Acad. Sci. USA 110, 5689.
Product Information
FormOff-white powder
Hill FormulaC₂₁H₁₇F₃N₄
Chemical formulaC₂₁H₁₇F₃N₄
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetFMS
Secondary targetKIT
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 Ambient Temperature Only
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
Katalógusszám GTIN
505146 0

Documentation

FMS/KIT Dual Kinase Inhibitor, PLX647 - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

References

Hivatkozások áttekintése
Zhang, C., et al. 2013. Proc. Natl. Acad. Sci. USA 110, 5689.

Brochure

Title
New Products Flyer- Feb 2014 - Vol 1
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.

Revision27-September-2013 JSW
SynonymsCDC2L6/CDK11/CDK19 Inhibitor, CDK8 Inhibitor, cFMS Inhibitor V, CSF-1 Receptor Inhibitor V, CSF1R Inhibitor V, DDR2 Inhibitor II, Flt-3 Inhibitor VIII, IL-34 Receptor Inhibitor V, NTRK3/TrkC Inhibitor, VEGFR Tyrosine Kinase Inhibitor XXXVI, VEGFR2 Tyrosine Kinase Inhibitor XXXIV, c-Kit Inhibitor IV, PLX-647
DescriptionA cell-permeable and bio-available azaindolylmethylpyridamine derivative that acts as a potent inhibitor against FMS and KIT (IC50 = 28 and 16 nM, respectively) by targeting and locking these two PDGF family receptor kinases in their inactive DGF-out conformation, while being less effective against Flt3, KDR/VEGFR2, CDC2L6/CDK11/CDK19, NTRK3/TrkC, DDR2, CDK8/cyclin C (IC50 = 91, 130, 350, 620, 700, and 710 nM, respectively) and exhibiting much reduced or little potency toward other kinases in a 400-kinase panel selectivity study (IC50 >1 µM). Shown to effectively inhibit CSF-1-induced (with RANKL as co-stimulator) osteoclast differentiation (IC50 = 170 nM), cellular FLT3-ITD, FMS, KIT phosphorylations (IC50 ranges from 20 to 250 nM), as well as FLT3-ITD-, FMS-, KIT-dependent proliferations (IC50 ranges from 92 to 380 nM), while being less effective against KDR- or wt FLT3-dependent proliferations (IC50 ranges from 1.6 to 5 µM). Orally available in rats (AUC0-∞ (h·µg/mL)/Cmax (µg/mL) = 6.4/0.63 and 46.35/3.72 post 10 mg/kg and 40 mg/kg oral dosage, respectively) and mice (AUC0-∞ (h·µg/mL)/Cmax (µg/mL) = 8.51/1.67 and 53.3/7.78 post 10 mg/kg and 40 mg/kg oral dosage, respectively) and is reported to exhibit in vivo efficacy in preventing rat MRMT-1 breast carcinoma bone metastases-caused osteolysis (30 mg/kg b.i.d.) as well as in blocking inflammation responses in several murine models, including UUO- (unilateral ureter obstruction) induced kidney inflammation (40 mg/kg b.i.d.), collagen-induced arthritis (20 to 80 mg/kg b.i.d.), LPS-induced serum IL-6 & TNF-α release (single 40 mg/kg oral dose 4.25 h before LPS), and mast cell activation-induced anaphylaxis (single 80 mg/kg oral dose 2 h before antigen stimulation).
FormOff-white powder
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₂₁H₁₇F₃N₄
Structure formulaStructure formula
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
ReferencesZhang, C., et al. 2013. Proc. Natl. Acad. Sci. USA 110, 5689.