2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. HSP
  4. CH5138303

CH5138303 是一种口服有效的 Hsp90 抑制剂。CH5138303 与 Hsp90α N 端具有较高的结合亲和力，Kd 为 0.52 nM。CH5138303 对人癌细胞 (HCT116 和 NCI-N87) 具有较强的抗增殖活性，其 IC50 值分别为 0.098 和 0.066 μM。CH5138303 小鼠口服生物利用度高 (F=44.0%)。CH5138303 在人 NCI-N87 胃癌异种移植模型中显示出强大的抗肿瘤作用。

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CH5138303 Chemical Structure

CH5138303 Chemical Structure

CAS No. : 959763-06-5

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规格 价格 是否有货 数量
1 mg ￥2800
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Customer Review

CH5138303 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

CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model[1][2].

IC50 & Target

HSP90α

0.52 nM (Kd)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HCT-116 IC50
0.098 μM
Compound: 16l, CH5138303
Cytotoxicity against human HCT116 cells after 4 days by CCk-8 assay
Cytotoxicity against human HCT116 cells after 4 days by CCk-8 assay
[PMID: 24369839]
NCI-N87 IC50
0.066 μM
Compound: 16l, CH5138303
Cytotoxicity against human NCI-N87 cells after 4 days by CCk-8 assay
Cytotoxicity against human NCI-N87 cells after 4 days by CCk-8 assay
[PMID: 24369839]
NCI-N87 ED50
3.9 mg/kg
Compound: 16l, CH5138303
Antitumor activity against human NCI-N87 cells xenografted in po dosed BALB/c nu/nu mouse assessed as tumor growth inhibition administered qd for 11 days
Antitumor activity against human NCI-N87 cells xenografted in po dosed BALB/c nu/nu mouse assessed as tumor growth inhibition administered qd for 11 days
[PMID: 24369839]
体外研究
(In Vitro)

When used in combination with FLC, CH5138303 shows antifungal activitiy against azole-resistant C. albicans, with a FICI (fractional inhibitory concentration index) of 0.500[2].

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

CH5138303 相关抗体:
体内研究
(In Vivo)

CH5138303 (SCID mice bearing NCI-N87 cells, 0-50 mg/kg, Orally, once daily for 11 days) shows potent antitumor efficacy with TGI (tumor growth inhibition) of 136% and a median effective dose (ED50) of 3.9 mg/kg without significant loss of body weight[1].

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

415.90

Formula

C19H18ClN5O2S
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

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 33 mg/mL (79.35 mM; 超声加热助溶; 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 2.4044 mL 12.0221 mL 24.0442 mL
5 mM 0.4809 mL 2.4044 mL 4.8088 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, 6 months; -20°C, 1 month (protect from light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 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: 99.05%

COA (196 KB) HNMR (211 KB) RP-HPLC (230 KB)

产品使用指南 (1538 KB)
参考文献

CH5138303 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, 6 months; -20°C, 1 month (protect from light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4044 mL 12.0221 mL 24.0442 mL 60.1106 mL
5 mM 0.4809 mL 2.4044 mL 4.8088 mL 12.0221 mL
10 mM 0.2404 mL 1.2022 mL 2.4044 mL 6.0111 mL
15 mM 0.1603 mL 0.8015 mL 1.6029 mL 4.0074 mL
20 mM 0.1202 mL 0.6011 mL 1.2022 mL 3.0055 mL
25 mM 0.0962 mL 0.4809 mL 0.9618 mL 2.4044 mL
30 mM 0.0801 mL 0.4007 mL 0.8015 mL 2.0037 mL
40 mM 0.0601 mL 0.3006 mL 0.6011 mL 1.5028 mL
50 mM 0.0481 mL 0.2404 mL 0.4809 mL 1.2022 mL
60 mM 0.0401 mL 0.2004 mL 0.4007 mL 1.0018 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:

CH5138303959763-06-5CH 5138303CH-5138303HSPHeat shock proteinsorally activeantitumor agentHsp90 inhibitorHCT116NCI-N87gastric cancerInhibitorinhibitorinhibit

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