PF-04929113 Mesylate

CAS No.	1173111-67-5	Cat. No.	BCP17210
Name	PF-04929113 Mesylate
Synonyms	PF04929113 Mesylate;PF 04929113 Mesylate;SNX5422 Mesylate;SNX-5422 Mesylate;SNX 5422 Mesylate;
Formula	C26H34F3N5O7S	M. Wt	617.64

Description	in vitro: PF-04929113 is a small-molecule Hsp90 inhibitor based on the 6,7-dihydro-indazol-4-one scaffold. PF-04929113 developed by Serenex, converts to SNX-2122, which is the active Hsp90 inhibitor form. PF-04929113 exhibits potent effects on Her-2 stability and causes expected up-regulation of Hsp70. PF-04929113 shows potent antiproliferative activity against a broad range of cancer cell types, e.g. MCF-7 (IC50=16 nM), SW620 (IC50=19 nM), K562 (IC50=23 nM), SK-MEL-5 (IC50=25 nM), and A375 (IC50=51 nM). in vivo: PF-04929113 inhibits human MM cell growth in vivo, and immuno-histochemical analysis shows PF-04929113 significantly inhibits p-ERK and p-Akt in treated mice. Meanwhile, PF-04929113 treatment significantly decreases the percentage of CD31+ cells and MVD, consistent with an inhibitory effect on angiogenesis in vivo. A 50 mg/kg administration of PF-04929113 delivered 3 times per week significantly delays castrate-resistant LNCaP tumor growth and prolongs cancer specific survival
Pathways	Protease/Metabolic Enzyme Cell Cycle/DNA Damage
Targets	HSP

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