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VER-49009

SKU: orb1221619

Description

VER-49009 is a potent HSP90 inhibitor. VER-49009 inhibits Hsp90 with an IC50 value of 47 nM. VER-49009 produces a cellular antiproliferative GI50 value of 685 nM when tested against a human cancer cell line panel. Consistent with inhibition of Hsp90, VER-49009 induces the expression of Hsp27 and Hsp72 while reducing the client proteins C-RAF, B-RAF, survivin, and PRMT5, causing cell cycle arrest and apoptosis.

Images & Validation

Key Properties

CAS Number558640-51-0
MW387.82
Purity>98% (HPLC)
FormulaC19H18ClN3O4
SMILESc1(c(cc(c(c1)c1c(c([nH]n1)C(=O)NCC)c1ccc(cc1)OC)O)O)Cl
TargetFactor Xa
SolubilityDMSO : 100 mg/mL 257.85 mM;H2O : < 0.1 mg/mL

Bioactivity

In Vivo
VER-49009 (4 mg/kg, i.p.) results in clear depletion of ERBB2 at 3 and 8 h following the final dose, with client protein levels returning to normal by 24 h, in the athymic mice bearing well-established OVCAR3 human ovarian ascites tumors.
In Vitro
VER-49009 is a Hsp90 inhibitor, with an IC50 of 25 nM. VER-49009 binds to the ATPase of full length yeast Hsp90 protein, with an IC50 of 140 nM. VER-49009 inhibits Hsp90, with a Kd of 78 nM. VER-49009 also shows antiproliferative activities against various human cancer cells, with a mean GI50 of 685 ± 119 nM. VER-49009 suppressses the proliferation of human umbilical vein endothelial cells (HUVEC) with GI50 values of 444 ± 91.1 nM, and shows higher GI50s against nontumorigenic human breast (MCF10a) and prostate (PNT2) epithelial cells. VER-49009 displays no differences in cellular activities of isogenic cell lines, and these activities are independent of NQO1 expression. VER-49009 inhibits the proliferation (1, 2.5 μM), induces G2 phase arrest and reduces total Akt and phospho-Akt expression levels in CFSC cells (1-5 μM).

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

VER49009 | VER 49009 | VER-49009

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VER-49009 (orb1221619)

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Available Sizes

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2 mg
$ 110.00
5 mg
$ 160.00
10 mg
$ 230.00
25 mg
$ 390.00
50 mg
$ 610.00
100 mg
$ 830.00
200 mg
$ 1,150.00
500 mg
$ 1,660.00