ChemicalBook CAS DataBase List 5-(1H-Pyrrolo[2,3-b]pyridin-3-ylmethyl)-N-[[4-(trifluoromethyl)phenyl]methyl]-2-pyridinamine dihydrochloride

5-(1H-Pyrrolo[2,3-b]pyridin-3-ylmethyl)-N-[[4-(trifluoromethyl)phenyl]methyl]-2-pyridinamine dihydrochloride

Product Name5-(1H-Pyrrolo[2,3-b]pyridin-3-ylmethyl)-N-[[4-(trifluoromethyl)phenyl]methyl]-2-pyridinamine dihydrochloride
CAS1779796-38-1
CBNumberCB84902809
MFC21H18ClF3N4
MW418.85
MDL NumberMFCD27991296
MOL File1779796-38-1.mol

5-(1H-Pyrrolo[2,3-b]pyridin-3-ylmethyl)-N-[[4-(trifluoromethyl)phenyl]methyl]-2-pyridinamine dihydrochloride Price

Product number	Packaging	Price	Product description	Buy
Usbiological 256284	10mg	$480	PLX 647 dihydrochloride	Buy

5-(1H-Pyrrolo[2,3-b]pyridin-3-ylmethyl)-N-[[4-(trifluoromethyl)phenyl]methyl]-2-pyridinamine dihydrochloride Chemical Properties,Usage,Production

Uses

PLX647 dihydrochloride is an orally active, highly specific dual FMS and KIT kinase inhibitor, with IC50s of 28 and 16 nM, reapectively. PLX647 dihydrochloride shows selectivity for FMS and KIT over a panel of 400 kinases at a concentration of 1 μM except FLT3 and KDR (IC50s=91 and 130 nM, respectively)[1].

in vivo

PLX647 dihydrochloride (40 mg/kg; p.o.; twice daily for 7 days) reduces macrophage accumulation in UUO kidney and blood monocytes^[1].
PLX647 dihydrochloride (40 mg/kg; p.o.; male Swiss Webster mice) reduces LPS-induced TNF-α and IL-6 release^[1].
PLX647 dihydrochloride (20-80 mg/kg; p.o.; daily or twice daily from 27-41 days) shows effects on collagen-induced arthritis^[1].
PLX647 dihydrochloride (30 mg/kg) results in significant inhibition of TRAP5b immunostaining and bone osteolysis. PLX647 dihydrochloride (30 mg/kg BID) is able to prevent bone damage by the tumor cells^[1].

Animal Model:	Male C57BL/6 mice (mouse unilateral ureter obstruction model)^[1]
Dosage:	40 mg/kg
Administration:	P.o.; twice daily for 7 days
Result:	Resulted in reduction in the levels of F4/80+ macrophages by 77%.

Animal Model:	7-9 wk old Male DBA/1J mice (Mouse collagen-induced arthritis model)^[1]
Dosage:	20 mg/kg, 80 mg/kg
Administration:	P.o.; daily (20 mg/kg) from 27-41 days, twice daily (80 mg/kg) from 27-41 days
Result:	20 mg/kg PLX647 had no initial effect on the development of severe arthritis. However, starting on day 33, no further development of disease severity was recorded, and a 30% inhibition of the macroscopic signs of arthritis was evident in clinical score on day 41. Mice treated with 80 mg/kg BID PLX647 initially shows delayed development of severe arthritic signs. Starting on day 33, the signs of arthritis began to decrease in this treatment group, reaching a maximum reversal of 76% on day 41.

References

[1] Zhang C, et al. 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

Preparation Products And Raw materials

5-(1H-Pyrrolo[2,3-b]pyridin-3-ylmethyl)-N-[[4-(trifluoromethyl)phenyl]methyl]-2-pyridinamine dihydrochloride Suppliers

Supplier	Tel	Email	Country	ProdList	Advantage
Nantong HI-FUTURE Biology Co., Ltd.	+undefined18051384581	sales@chemhifuture.com	China	3135	58
Shanghai Hongye Biotechnology Co. Ltd	400-9205774	sales@glpbio.cn	China	6777	58
Nantong Hi-Future Biotechnology Co., Ltd	18051384581	sales@chemhifuture.com	China	2997	58
TargetMol Chemicals Inc.	4008200310	marketing@tsbiochem.com	China	24961	58
Biosynth Biological Technology (Suzhou) Co Ltd	51288865780	sales@biosynth.com	China	6051	58

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