2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. HSP
  4. BX-2819

BX-2819 是 Hsp90 抑制剂 IC50 值为 41 nM。BX-2819 能够抑制癌细胞的增殖。BX-2819 可显著抑制裸鼠 NCI-N87 和 HT-29 肿瘤的生长。

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BX-2819 Chemical Structure

BX-2819 Chemical Structure

CAS No. : 1184181-50-7

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BX-2819 相关抗体

Top Publications Citing Use of Products

查看 HSP 亚型特异性产品:

查看所有亚型
HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BX-2819 is a Hsp90 inhibitor with an IC50 value of 41 nM. BX-2819 inhibits the proliferation of cancer cells. BX-2819 can significantly inhibit the growth of NCI-N87 and HT-29 tumors in nude mice[1].

IC50 & Target[1]

HSP90

41 nM (IC50)

HSP70

 

体外研究
(In Vitro)

BX-2819 (0.001-10 μM, 16 h) 在 HT-29 、OVCAR3、 SKBR3 细胞中能够抑制 ErbB2 蛋白的表达,显著增强 Hsp70 的表达[1]。
BX-2819 (72 h) 在SKBR3 (IC50=14 nM), SKOV3 (IC50=36 nM), MKN45 (IC50=72 nM), NCI-N87 (IC50=7 nM) 肿瘤癌细胞中能够抑制细胞增殖[1]。
BX-2819 (100 μM, 72 h) 在 HepG2 和 RPTEC 细胞中对细胞没有明显的毒性作用[1]。

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

BX-2819 相关抗体:

Western Blot Analysis[1]

Cell Line: NCI-N87, MKN-45
Concentration: 0.001 μM, 0.01 μM, 0.1 μM, 1 μM, 10 μM
Incubation Time: 16 h
Result: Significantly inhibited the expression of ErbB2, Raf1 and c-Met proteins.
体内研究
(In Vivo)

BX-2819 (100 mg/kg, 腹腔注射 (i.p.), 每周两次) 在 NCI-N87 和 SKOV3 肿瘤小鼠中能够显著抑制 ErbB2 蛋白的表达。在 HT-29 和 NCI-N87 肿瘤小鼠中，显著降低了肿瘤生长和最终肿瘤负荷[1]。
BX-2819 (2 mg/kg, 静脉注射 (i.v.), 单剂量) 在小鼠中的血清半衰期相对较短 (t1/2 = 0.8 h)，清除率较高 (CL = 159 mL / min / kg)，分布体积较大(Vss = 4.5 L)[1]。

在小鼠中 BX-2819 的药代动力学分析[1]

Dose（mg/kg） Route T1/2(h) AUCinf(μg h/mL) CL (mL/min) Vss(L/kg)
2 iv 0.8 0.23 159 4.5

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

Animal Model: SKOV3, HT-29 and NCI-N87 xenograft models in nude mice[1]
Dosage: 100 mg/kg
Administration: Intraperitoneal injection (i.p.), twice a week
Result: Significantly inhibited ErbB2 expression, effectively inhibited Hsp90 for a long time, and enhanced Hsp70 expression.
Could enter the plasma after intraperitoneal injection.
Significantly decreased in tumor growth and final tumor burden.
分子量

428.50

Formula

C21H24N4O4S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

BX-2819 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

BX-28191184181-50-7BX2819BX 2819HSPHeat shock proteinsHsp90NCI-N87HT-29 SKBR3SKOV3MKN45HT-29HepG2RPTECColon cancerOvarian cancerInhibitorinhibitorinhibit

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目录号：
HY-157085
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