PLX-647


Catalog No. size PriceQuantity
M6408-2 2mg solid $105
M6408-10 10mg solid $431

Description

Cas:873786-09-5

Product Information

PLX-647 is PLX647 is a potent inhibitors of both FMS and KIT that show strong selectivity compared with other kinases. In the in vitro enzymatic assay, PLX647 inhibits FMS with IC50 = 0.028μM and KIT with IC50 = 0.016 μM. PLX647 represents a unique class of kinase inhibitors with unique dual FMS and KIT specificity.

 

Chemical Formula: C21H17F3N4

 

Exact Mass: 382.14053

 

Molecular Weight: 382.38

 

Elemental Analysis: C, 65.96; H, 4.48; F, 14.91; N, 14.65

 

Synonym:

 

PLX647

PLX 647

PLX-647

 

Chemical Name: 5-((1H-pyrrolo[2,3-b]pyridin-3-yl)methyl)-N-(4-(trifluoromethyl)benzyl)pyridin-2-amine

 

InChi Key:

NODCQQSEMCESEC-UHFFFAOYSA-N

 

InChi Code: InChI=1S/C21H17F3N4/c22-21(23,24)17-6-3-14(4-7-17)11-26-19-8-5-15(12-27-19)10-16-13-28-20-18(16)2-1-9-25-20/h1-9,12-13H,10-11H2,(H,25,28)(H,26,27)

 

Smiles Code:

FC(C1=CC=C(C=C1)CNC2=NC=C(CC3=CNC4=NC=CC=C43)C=C2)(F)F

 

 

Technical Data:

 

Appearance: white solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

In Vitro:

In vitro, PLX647 potently inhibits proliferation of BCR-FMS cells, with an IC50 of 92 nM. A corresponding Ba/F3 cell line expressing BCR-KIT is also quite sensitive to PLX647, with an IC50 of 180 nM. PLX647 also inhibits endogenous FMS and KIT, as demonstrated by inhibition of the ligand-dependent cell lines M-NFS-60 (IC50=380 nM) and M-07e (IC50=230 nM), which express FMS and KIT, respectively.

PLX647 potently inhibits the growth of FLT3–ITD-expressing MV4-11 cells (IC50=110 nM). PLX647 displayed minimal inhibition of the proliferation of Ba/F3 cells expressing BCR–KDR (IC50=5 μM). PLX647 inhibits osteoclast differentiation with an IC50 of 0.17 μM.

 

In Vivo:

PLX647 (40 mg/kg; p.o.; twice daily for 7 days) reduces macrophage accumulation in UUO kidney and blood monocytes.

PLX647 (40 mg/kg; p.o.; male Swiss Webster mice) reduces LPS-induced TNF-α and IL-6 release.

PLX647 (20-80 mg/kg; p.o.; daily or twice daily from 27-41 days) shows effects on collagen-induced arthritis.

PLX647 (30 mg/kg) results in significant inhibition of TRAP5b immunostaining and bone osteolysis. PLX647 (30 mg/kg BID) is able to prevent bone damage by the tumor cells.

 

 

References

 

  1. Zhang C, Ibrahim PN, Zhang J, Burton EA, Habets G, Zhang Y, Powell B, West BL, Matusow B, Tsang G, Shellooe R, Carias H, Nguyen H, Marimuthu A, Zhang KY, Oh A, Bremer R, Hurt CR, Artis DR, Wu G, Nespi M, Spevak W, Lin P, Nolop K, Hirth P, Tesch GH, Bollag G. Design and pharmacology of a highly specific dual FMS and KIT kinase inhibitor. Proc Natl Acad Sci U S A. 2013 Apr 2;110(14):5689-94. doi: 10.1073/pnas.1219457110. Epub 2013 Mar 14. PubMed PMID: 23493555; PubMed Central PMCID: PMC3619323.

 

  1. Louvet C, Szot GL, Lang J, Lee MR, Martinier N, Bollag G, Zhu S, Weiss A, Bluestone JA. Tyrosine kinase inhibitors reverse type 1 diabetes in nonobese diabetic mice. Proc Natl Acad Sci U S A. 2008 Dec 2;105(48):18895-900. doi: 10.1073/pnas.0810246105. Epub 2008 Nov 17. PubMed PMID: 19015530; PubMed Central PMCID: PMC2596241.

 

Products are for research use only. Not for human use.

 

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