PF-04929113

Research use only, not for human use.

PF-04929113 (SNX-5422) is a potent and selective HSP90 inhibitor with Kd of 41 nM and induces Her-2 degradation with IC50 of 37 nM. Phase 1/2.

PF-04929113 (SNX-5422) is a potent and selective HSP90 inhibitor with Kd of 41 nM and induces Her-2 degradation with IC50 of 37 nM. Phase 1/2.

SNX-5422 is an orally active Hsp90 inhibitor, with a Kd of 41 nM, and also induces Her-2 degradation, with an IC50 of 37?nM. SNX-5422 exhibits potent effects on Her2 and p-ERK stability in AU565 cells and p-S6 in A375 cells, with IC50s of 5?±?1, 11?±?3, and 61?±?22 nM, respectively. SNX-5422 also induces Hsp70 in A375 cells with an IC50 of 13?±?3 nM. SNX-5422 (SNX5422; 0.5, 1, 2, 5, and 10 μM) reduces cell viability in a concentration-dependent manner. Moreover, SNX-5422 (1, 3, 5, 7 μM) in combination with equal amounts of HDAC inhibitors (PXD101, SAHA, and TSA) synergistically induces cell death via suppression of PI3K/Akt/mTOR signaling in ATC cells.

SNX-5422 (50 mg/kg, p.o.) efficiently inhibits tumor growth of HT-29 human colon tumor xenograft model after administration 3 times a week for 3 weeks (qod×3/2×3). SNX-5422 (20, 40 mg/kg, p.o.) markedly inhibits multiple myeloma (MM) tumor growth and angiogenesis in mice.

SNX-5422

Angiogenesis

HER/HSP

HER2| HSP90

Cancer

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908115-27-5

521.53

C25H30F3N5O4

>98% (HPLC)

DMSO:104 mg/mL (199.41 mM); Ethanol:5 mg/mL (9.58 mM); Water:<1 mg/mL (<1 mM)

CC1(C)CC2=C(C(=NN2C2=CC=C(C(N)=O)C(N[C@H]3CC[C@@H](CC3)OC(=O)CN)=C2)C(F)(F)F)C(=O)C1 |r,c:6,30,t:4,10,12|

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(-20℃)

With Ice Pack

≥ 2 years