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VER-50589

SKU: orb1221819

Description

VER-50589 is a potent Hsp90 inhibitor. VER-50589 inhibits Hsp90 with an IC50 value of 21 nM. It produces a mean cellular antiproliferative GI50 value of 78 nM when tested against a human cancer cell line panel. VER-50589 shows favorable pharmacokinetics and impairs tumor growth in animals.

Images & Validation

Key Properties

CAS Number747413-08-7
MW388.8
Purity>98% (HPLC)
FormulaC19H17ClN2O5
SMILESc1(cc(c(cc1O)O)c1c(c2ccc(cc2)OC)c(no1)C(=O)NCC)Cl
TargetNF-κB
SolubilityDMSO : ≥ 48 mg/mL; 123.46 mM

Bioactivity

In Vivo
VER-50589 (4 mg/kg, i.p.) exerts a complete HSP90 inhibition in the athymic mice bearing well-established OVCAR3 human ovarian ascites tumors. VER-50589 (100 mg/kg, i.p.) shows reduced tumor volume and tumor weights in the HCT116 colon carcinoma xenografts compared to the control mice group.
In Vitro
VER-50589 is a Hsp90 inhibitor, with an IC50 of 21 nM and a Kd of 4.5 nM. VER-50589 inhibits intrinsic ATPase of full-length recombinant yeast Hsp90, with an IC50 of 143 ± 23 nM in the presence of 400 μM ATP. VER-50589 shows antiproliferative activities against various human cancer cells, with the lowest GI50 of 32.7 ± 0.2 nM for CH1 human ovarian cells, and mean GI50 of 78 ± 15 nM. VER-50589 suppressses the proliferation of human umbilical vein endothelial cells (HUVEC) with GI50 value of 19 ± 2.4 nM, and shows higher GI50s against nontumorigenic human breast (MCF10a) and prostate (PNT2) epithelial cells. Furthermore, VER-50589 displays no differences in cellular activities of isogenic cell lines, and these activities are independent of NQO1 expression. VER-50589 also causes G1 and G2-M block (115 or 575 nM) and induces cytostasis in HCT116 colon cancer cells. In addition, VER-50589 causes great uptake in HCT116 cells.

Storage & Handling

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

Alternative Names

VER50589 | VER 50589 | VER-50589

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VER-50589 (orb1221819)

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200 mg
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$ 120.00
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100 mg
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