2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. HSP CDK
  4. Hsp90-IN-46

Hsp90-IN-46 是一种 Hsp90 抑制剂。Hsp90-IN-46 对肿瘤细胞株具有广谱抗增殖活性。Hsp90-IN-46 通过减少集落形成、下调增殖标志物 Ki-67 来抑制乳腺癌细胞增殖。Hsp90-IN-46 可抑制 Hsp90 及其 ATP 酶活性，下调下游底物癌蛋白 HER2 与 CDK4，并适度诱导热休克反应。Hsp90-IN-46 在三阴性乳腺癌肿瘤异种移植小鼠模型中具有显著的抗肿瘤活性。Hsp90-IN-46 可用于三阴性乳腺癌、白血病、非小细胞肺癌、结肠癌、卵巢癌、肾癌、前列腺癌等多种癌症的研究。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Hsp90-IN-46

Hsp90-IN-46 Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

Hsp90-IN-46 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

查看 CDK 亚型特异性产品:

查看所有亚型
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Hsp90-IN-46 is a Hsp90 inhibitor. Hsp90-IN-46 exhibits broad-spectrum antiproliferative activity against tumor cell lines. Hsp90-IN-46 inhibits breast cancer cell proliferation by reducing colony formation and downregulating the proliferation marker Ki-67. Hsp90-IN-46 inhibits Hsp90 and its ATPase activity, downregulates the downstream substrate oncoproteins HER2 and CDK4, and moderately induces the heat shock response. Hsp90-IN-46 shows significant antitumor activity in a mouse model of triple-negative breast cancer tumor xenografts. Hsp90-IN-46 can be used for research on various cancers including triple-negative breast cancer, leukemia, non-small cell lung cancer, colon cancer, ovarian cancer, renal cancer, prostate cancer[1].

IC50 & Target[1]

HSP90

 

体外研究
(In Vitro)

Hsp90-IN-46 (Compound 13b) (0.01-100 μM; 48 h) 在 48 种人类肿瘤细胞系中表现出强效、广谱的抗癌活性，其 GI50 值范围为 2.17 至 9.60 μM，可在 26 种细胞系中实现总生长抑制，且在 5 种浓度下作用 48 h 的测试中，对大多数细胞系的致死性极低[1]。
Hsp90-IN-46 (48 h) 对 MCF-7 和 MDA-MB-231 乳腺癌细胞系具有高活性和选择性抑制作用，其 IC50 值分别为 1.33 μM 和 1.95 μM[1]。
Hsp90-IN-46 (1-5 μM, 9 days) 抑制 MDA-MB-231 乳腺癌细胞增殖，降低 MCF-7 和 MDA-MB-231 乳腺癌细胞中增殖标志物 Ki67 的表达，下调 Hsp90 底物癌蛋白 HER2 和 CDK4 的表达[1]。
Hsp90-IN-46 可在基于体外 AlphaLISA 的分析实验中直接抑制 Hsp90 的活性，其 IC50 为 12.397 μM，可在偶联分光光度法测定中强效抑制 Hsp90 ATP 酶活性，其 IC50 为 0.986 μM[1]。
Hsp90-IN-46 (10 μM) 可在 HEK-293 细胞中诱导中度热休克反应，在 10 μM 浓度下使 HspA1A mRNA 表达水平升高 8.7 倍[1]。

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

Hsp90-IN-46 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: 48 human tumor cell lines from multiple subpanels (NSCLC, colon, CNS, melanoma, ovarian, renal, prostate, leukemia, breast)
Concentration: 10 μM
Incubation Time: 48 h
Result: Exhibited a mean growth inhibition (GI%) of 78.84% across 48 cell lines.
Showed strong cytotoxicity (GI% 57.74-68.93%) against NSCLC (NCI-H226), colon (HCC-2998, HT29, SW-620), CNS (SF-539), melanoma (M14), ovarian (OVCAR-3, OVCAR-8), renal (A498, RXF 393), and prostate (DU-145) cancer cell lines.
Demonstrated potent cytotoxicity (GI% 70.24-97.44%) against all leukemia cell lines and most NSCLC, melanoma, colon, CNS, ovarian, renal, and breast cancer cell lines.
Induced 56.97% and 4.33% lethality against melanoma SK-MEL-5 and SK-MEL-2 cell lines, respectively.

Cell Cytotoxicity Assay[1]

Cell Line: 60 human tumor cell lines
Concentration: 0.01-100 μM
Incubation Time: 48 h
Result: Demonstrated potent cytotoxicity with GI50 values of 2.17-9.60 μM against 48 cell lines.
Showed lower activity with GI50 values of 10.20-22.70 μM against 12 cell lines.
Induced total growth inhibition (TGI) with values of 6.23-91.00 μM against 26 cell lines (including breast MDA-MB-468, melanoma SK-MEL-5, UACC-62, SK-MEL-2, and ovarian OVCAR-3).
Exhibited minimal toxicity with LC50 >92.5 μM against 57 cell lines, except LC50 values of 27.40-61.30 μM against colon COLO 205 and melanoma SK-MEL-5, UACC-62 cell lines.
Achieved a full-panel GI50 mean graph-midpoint (MG-MID) value of 5.89 μM, with breast cancer MDA-MB-468 as the most sensitive cell line (GI50 = 2.17 μM) and ovarian cancer OVCAR-5 as the least sensitive (GI50 = 22.7 μM).

Cell Cytotoxicity Assay[1]

Cell Line: MCF-7, MDA-MB-231, Caco-2, A549 cancer cell lines; normal human skin fibroblast (HSF) cells
Concentration: Serial concentrations
Incubation Time: 48 h
Result: Displayed IC50 values of 1.33 μM (MCF-7), 1.95 μM (MDA-MB-231), 4.62 μM (Caco-2), 11.89 μM (A549), and 46.96 μM (HSF).
Achieved selectivity index values of 35.31 (MCF-7), 24.08 (MDA-MB-231), 10.16 (Caco-2), and 3.95 (A549).

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231 breast cancer cells
Concentration: 5 μM
Incubation Time: 9 days
Result: Significantly reduced colony formation from 173 colonies per well (control) to 91 colonies per well.
药代动力学
(Parmacokinetics)
Species Dose Route Cmax Tmax T1/2 AUC
Rat[1] 50 mg/kg i.p. 6.74 ± 1.28 μM 1 h 2.98 h 30.68
体内研究
(In Vivo)

Hsp90-IN-46 (13b) (50 mg/kg; i.p.; daily; 6 consecutive days) 在三阴性乳腺癌肿瘤异种移植小鼠模型中具有显著的抗肿瘤活性[1]。

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

Animal Model: BALB/c mice (immunocompromised)[1]
Dosage: 50 mg/kg
Administration: i.p.; daily; 6 consecutive days
Result: Reduced MDA-MB-231 xenograft tumor volume and tumor weight by approximately 33%.
Reduced EGFR expression in tumor sections to 0.17-0.92% reaction area.
Maintained stable body weight in treated mice.
分子量

468.30

Formula

C21H18BrN5O3
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

Hsp90-IN-46 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:

Hsp90-IN-46HSPCDKHeat shock proteinsCyclin dependent kinaseHsp90 inhibitortriple-negative breast cancerleukemianon-small cell lung cancercolon cancerovarian cancerrenal cancerprostate cancerbreast cancerMCF-7 cellsMDA-MB-231 cellsBALB/c miceInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
Hsp90-IN-46
目录号：
HY-181687
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z