2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. HSP
  4. VER-82576

VER-82576  (Synonyms: NVP-BEP800)

目录号: HY-10942 纯度: 98.76%
COA 产品使用指南

摩尔计算器

VER-82576 (NVP-BEP800) 是一种有效的，可口服的，选择性的 Hsp90 抑制剂，对 Hsp90β 的 IC50 值为 58 nM；VER-82576 同时可较弱地抑制 Grp94 和 Trap-1 的活性，IC50 值分别为 4.1 和 5.5 μM。

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VER-82576 Chemical Structure

VER-82576 Chemical Structure

CAS No. : 847559-80-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1100
In-stock
1 mg ￥454
In-stock
5 mg ￥1000
In-stock
10 mg ￥1800
In-stock
50 mg ￥5600
In-stock
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

VER-82576 相关抗体

Top Publications Citing Use of Products

查看 HSP 亚型特异性产品:

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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

VER-82576 (NVP-BEP800) is a potent, orally available and selective Hsp90 inhibitor, with an IC50 of 58 nM for Hsp90β; VER-82576 also slightly blocks Grp94 and Trap-1, with IC50s of 4.1 and 5.5 μM, respectively.

IC50 & Target[1]

HSP90β

58 nM (IC50)

GRP94

4.1 μM (IC50)

TRAP-1

5.5 μM (IC50)

体外研究
(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[1]. 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[2]. 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[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

VER-82576 相关抗体:
体内研究
(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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

480.41

Formula

C21H23Cl2N5O2S
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 6.2 mg/mL (12.91 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0816 mL 10.4078 mL 20.8156 mL
5 mM 0.4163 mL 2.0816 mL 4.1631 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 98.76%

COA (201 KB) HNMR (185 KB) LCMS (323 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[3]

Prior to treatments, the cells are placed into 6-well plates in medium at a density of 1 × 105 cells/well, three wells per treatment group and cultured for 24 h. The cells are divided into treatment groups and treated accordingly for 40 h: vehicle control (DMSO, 0.016%, v/v), VER-82576 (0.05, 0.1 or 0.2 μM), irradiation (10 Gy), or VER-82576 (0.05, 0.1 or 0.2 μM) in combination with irradiation (10 Gy). Upon completion of the treatment, all cells are incubated with 0.5 mg/ml MTT for 3 h. The relative viability of the treated cells to the untreated control cells is measured. The absorbance is measured at 490 nm on a microplate reader[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

The estrogen receptor (ER)-positive, ErbB2-overexpressing cell line BT-474 is grown in DMEM high glucose (4.5 g/L) supplemented with 10% FCS, 200 mM l-glutamine, and 1% sodium pyruvate (BioConcept). Two or 3 d before cell inoculation, each mouse is s.c. implanted on the upper dorsal side with a 17β-estradiol pellet (25 μg/d; 90-d release) using a trocar needle. BT-474 cells (5 × 106) are injected in 200 μL Matrigel/HBSS (1:1 volume) s.c. in the right flank. The A375 cell line expresses mutant B-Raf (V600E). The cells are grown in RPMI 1640 supplemented with 10% FCS and 200 mM l-glutamine. To establish tumors, 5 × 106 A375 cells are injected s.c. in 200 μL PBS in the right flank. The animals are kept under optimized hygienic conditions with a 12-h dark, 12-h light cycle. The animals are fed food and water ad libitum. Tumor growth and body weights are monitored at regular intervals. The xenograft tumor sizes are measured manually with calipers, and the tumor volume is estimated using the following formula: (W × L × H × π/6), where width (W), length (L), and height (H) are the three largest diameters. Treatment with VER-82576 is initiated when the average tumor volume reaches 100 to 300 mm3[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

VER-82576 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0816 mL 10.4078 mL 20.8156 mL 52.0389 mL
5 mM 0.4163 mL 2.0816 mL 4.1631 mL 10.4078 mL
10 mM 0.2082 mL 1.0408 mL 2.0816 mL 5.2039 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

VER-82576847559-80-2NVP-BEP800VER82576VER 82576HSPHeat shock proteinsInhibitorinhibitorinhibit

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目录号：
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