2. Membrane Transporter/Ion Channel
  3. BCRP
  4. MBL-II-141

MBL-II-141 是一种强效的 ABCG2 抑制剂，IC50 为 0.11 μM。MBL-II-141 以非竞争性方式抑制 ABCG2 的转运功能，阻止 ABCG2 将底物 (例如 Irinotecan (HY-16562)) 泵出细胞，从而增加药物在细胞内的积累。MBL-II-141 对 ABCB1 (P-gp) 和 ABCC1 (MRP1) 没有影响，并且细胞毒性极低 (IG50 > 100 μM)。MBL-II-141 可用于研究肿瘤多重耐药 (MDR)。

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MBL-II-141

MBL-II-141 Chemical Structure

CAS No. : 1353747-12-2

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MBL-II-141 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MBL-II-141 is potent ABCG2 inhibitor with an IC50 of 0.11 μM. MBL-II-141 inhibits the transport function of ABCG2 in a non-competitive manner, preventing ABCG2 from pumping substrates (such as Irinotecan (HY-16562)) out of the cells, thereby increasing the accumulation of drugs within the cells. MBL-II-141 has no effect on ABCB1 (P-gp) and ABCC1 (MRP1) and has extremely low cytotoxicity (IG50 > 100 μM). MBL-II-141 can be used for the study of multidrug resistance (MDR) cancers[1][2].

体内研究
(In Vivo)

MBL-II-141 (10 mg/kg，腹腔注射，每周三次，持续50-87天) 与抗癌药物 Irinotecan (CPT-11) 联合使用，可完全抑制 90% 新鲜植入的 ABCG2 阳性肿瘤的生长[2]。
MBL-II-141 (10 mg/kg，腹腔注射，单剂量) 可降低 Irinotecan 的总表观清除率和胆汁清除率，并显著增加血液和脑组织中 Irinotecan 和 SN-38 的暴露浓度[1][2]。
MBL-II-141 (10-50 mg/kg，腹腔注射或灌胃，单剂量) 表现出相对较高的预测 LD50₅₀ (腹腔注射：290 mg/kg，口服：1200 mg/kg)，实验证实即使剂量达 50 mg/kg 也没有明显的毒性或组织损伤[2]。

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

Animal Model: HEK-ABCG2 or HEK-pcDNA3.1 cells transfer model established in SCID mice[2]
Dosage: 10 mg/kg alone or with 20 mg/kg Irinotecan (CPT-11)
Administration: Intraperitoneal injection (i.p.), three times a week for 50-87 days
Result: Completely inhibited ABCG2-negative tumors, but only delayed the growth of ABCG2-positive tumors in single-agent treatment.
Completely inhibited the growth of 90% of ABCG2-positive tumors and significantly prolonged the survival time of the mice in combined treatment.
Slowed down the growth rate of tumors, and prolonged the survival time of mice in the established tumor model (ABCG2-positive tumors grew to a diameter of 8 mm) in combined treatment.
分子量

547.40

Formula

C28H23BrN2O5
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

MBL-II-141 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

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Keywords:

MBL-II-1411353747-12-2BCRPBreast cancer resistance proteinABCG2MDR phenotypeInhibitorsChemosensitizationInhibitorinhibitorinhibit

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