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Merck

5.05146

FMS/KIT Dual Kinase Inhibitor, PLX647

Synonym(s):

FMS/KIT Dual Kinase Inhibitor, PLX647, 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, PLX-647, c-Kit Inhibitor IV

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About This Item

Empirical Formula (Hill Notation):
C21H17F3N4
CAS Number:
873786-09-5
Molecular Weight:
382.38
UNSPSC Code:
12352200

Key Documents

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assay

≥98% (HPLC)

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

off-white

solubility

DMSO: 100 mg/mL

storage temp.

−20°C

Quality Level

100

Biochem/physiol Actions

Cell permeable: yes
Primary Target
FMS
Reversible: yes
Secondary Target
KIT

Disclaimer

Toxicity: Standard Handling (A)

General description

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 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).

Other Notes

Zhang, C., et al. 2013. Proc. Natl. Acad. Sci. USA110, 5689.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C. Stock solutions are stable for up to 3 months at -20°C.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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