NVP-BEP800|2mg|K1302-上海高创化学科技有限公司

NVP-BEP800

参考价：¥1298

供货周期：

一周

品牌：

规格：

2mg

货号：

K1302

CAS号：

847559-80-2

SKU:K1302		M. Wt:480.41
Formula:C21H23Cl2N5O2S		Solubility:No
Purity:>99%		Storage:2 years at -20 degrees centigrade
CAS No.:847559-80-2		Synonyms:VER-82576
Chemical NameN/A

Description	NVP-BEP800
Targets	HSP90-beta
IC50	58 nM
In vitro	NVP-BEP800 is a novel, fully synthetic, orally bioavailable inhibitor that binds to the NH(2)-terminal ATP-binding pocket of Hsp90. NVP-BEP800 can inhibit HSP90beta with IC50 of 58 nM. NVP-BEP800 showed activity against a panel of human tumor cell lines at nanomolar concentrations. In A375 melanoma and BT-474 breast cancer cell lines, NVP-BEP800 induced client protein degradation (including ErbB2, B-Raf(V600E), Raf-1, and Akt) and Hsp70 induction.
In vivo	NVP-BEP800 showed activity against a panel of primary human xenografts at nanomolar concentrations.Oral administration of NVP-BEP800 was well tolerated and induced robust antitumor responses in tumor xenograft models, including regression in the BT-474 breast cancer model.In these tumor models, NVP-BEP800 modulated Hsp90 client proteins and downstream signaling pathways at doses causing antitumor activity. NVP-BEP800. effectively and specifically killed the majority of primary myeloma cells in coculture with bone marrow stromal cells and reliably entailed molecular consequences of Hsp90 blockade - such as survival pathway breakdown and client protein depletion - in multiple myeloma cells from cell lines as well as from patients.
Clinical Trials	N/A
Features	N/A

Description

NVP-BEP800

Targets

HSP90-beta

IC50

58 nM

In vitro

NVP-BEP800 is a novel, fully synthetic, orally bioavailable inhibitor that binds to the NH(2)-terminal ATP-binding pocket of Hsp90. NVP-BEP800 can inhibit HSP90beta with IC50 of 58 nM. NVP-BEP800 showed activity against a panel of human tumor cell lines at nanomolar concentrations. In A375 melanoma and BT-474 breast cancer cell lines, NVP-BEP800 induced client protein degradation (including ErbB2, B-Raf(V600E), Raf-1, and Akt) and Hsp70 induction.

In vivo

NVP-BEP800 showed activity against a panel of primary human xenografts at nanomolar concentrations.Oral administration of NVP-BEP800 was well tolerated and induced robust antitumor responses in tumor xenograft models, including regression in the BT-474 breast cancer model.In these tumor models, NVP-BEP800 modulated Hsp90 client proteins and downstream signaling pathways at doses causing antitumor activity. NVP-BEP800. effectively and specifically killed the majority of primary myeloma cells in coculture with bone marrow stromal cells and reliably entailed molecular consequences of Hsp90 blockade - such as survival pathway breakdown and client protein depletion - in multiple myeloma cells from cell lines as well as from patients.

Clinical Trials

N/A

Features

N/A