NVP-BEP800

SKU: orb1223870

Description

A potent and selective Hsp90β inhibitor with IC50 of 58 nM; shows >70-fold selective against Grp94 and Trap-1; induces ErbB2, B-Raf(V600E), Raf-1, Akt and Hsp70 induction in A375 melanoma and BT-474 breast cancer cell lines; orally bioactive.Breast Cancer Preclinical.

Images & Validation

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Key Properties

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CAS Number	847559-80-2
MW	480.4106
Purity	>98% (HPLC)
Formula	C₂₁H₂₃Cl₂N₅O₂S
SMILES	O=C(C1=CC2=C(C3=CC(OCCN4CCCC4)=C(Cl)C=C3Cl)N=C(N)N=C2S1)NCC
Target	HSP
Solubility	DMSO: 6.2 mg/mL (Need ultrasonic)

Bioactivity

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In Vivo

VER-82576 (NVP-BEP800; 15 or 30 mg/kg, p.o.) shows antitumor activities in A375 cancer xenografts and BT-474 xenograft-bearing mice.

In Vitro

VER-82576 (NVP-BEP800) is a potent and selective Hsp90 inhibitor, with an IC50 of 58 nM for Hsp90β and is >70-fold selective against Grp94 and Trap-1, with IC50s of 4.1 ± 1.1 and 5.5 ± 0.48 μM. VER-82576 potently inhibits the proliferation of tumor cells, with GI50s ranging from 38 nM in A375 cells to 1050 nM in PC3 cells, with an average GI50 of 245 nM. VER-82576 (250-1250 nM) depletes client proteins in human cancer cell lines in vitro. VER-82576 (NVP-BEP800; 200 nM) shows no significant effect on the ionizing radiation (IR) dose-response curves of A549 cells, and is less toxic to SNB19 cells. VER-82576 in combination with IR results in more severe DNA damage in both A549 and SNB19 cell lines than each treatment alone and also protracts the kinetics of DNA damage repair in SNB19 cells. VER-82576 (NVP-BEP800; 0.05, 0.1 or 0.2 μM) dose-dependently decreases the viability and induces apoptosis of glioblastoma cells. VER-82576 (0.2 μM) suppresses the expression of IKKβ protein but does not alter the levels of IKKβ mRNA in T98G cells. VER-82576 (0.2 μM) suppresses the expression of heat shock protein 70.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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VER-82576 | VER82576

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HSP

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NVP-BEP800 (orb1223870)

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Purity:	98.87%
CAS Number:	847559-80-2
MW:	480.41
Formula:	C₂₁H₂₃Cl₂N₅O₂S

NVP-BEP800

Description

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

Similar Products

VER-82576 [orb1306450]

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NVP-BEP800 (orb1223870)

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