1. Membrane Transporter/Ion Channel
  2. BCRP
  3. MRS8432

MRS8432 是一种 ABCG2 调节剂,对人源 ABCG2EC50 为 7.5 nM。\nMRS8432 可激活 ABCG2 ATPase 活性。MRS8432 可部分抑制 ABCG2 介导的底物转运。MRS8432 可用于癌症多药耐药相关研究。

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MRS8432

MRS8432 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MRS8432 is an ABCG2 modulator with an EC50 of 7.5 nM against human ABCG2. MRS8432 activates ABCG2 ATPase activity. MRS8432 partially inhibits ABCG2-mediated substrate transport. MRS8432 is applicable to research related to cancer multidrug resistance[1].

体外研究
(In Vitro)

MRS8432 (0.1-10 μM; 20 min at 37°C) 可强效刺激 High-Five 昆虫细胞膜中 ABCG2 ATPase 的活性,其 EC50 为 7.5 nM[1]
MRS8432 (10 μM) 可在 HEK293-R5 细胞中部分抑制 ABCG2 介导的米托蒽醌和脱镁叶绿酸 A 的外排,测试浓度为 10 μM[1]
MRS8432 (up to 50 μM; 72 h) 在 HEK293-pcDNA 细胞和表达 ABCG2 的 HEK293-R5 细胞中显示出低细胞毒性 (IC50 >25 μM),且并非 ABCG2 介导的外排作用的底物[1]
MRS8432 以不结合 T402 残基的自折叠构象结合 ABCG2 药物结合口袋,与其对 ABCG2 ATPase 活性的刺激作用一致[1]

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

Cell Cytotoxicity Assay[1]

Cell Line: HEK293-pcDNA control cells, ABCG2-expressing HEK293-R5 cells
Concentration: Up to 50 μM
Incubation Time: 72 h
Result: Exhibited IC50 values for cytotoxicity >25 μM in both HEK293-pcDNA and HEK293-R5 cells.
Showed overlapping viability curves indicating MRS8432 is not transported by ABCG2.
分子量

694.09

Formula

C35H26ClF2N9O3

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
  • 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.

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产品名称:
MRS8432
目录号:
HY-181803
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