2. Cell Cycle/DNA Damage
  3. Folate Receptor (FR)
  4. 4A-BFA-11

4A-BFA-11 是一种叶酸靶向 PEG-MMAE 偶联物，对叶酸受体 α (FR-α) 具有特异性结合亲和力 (KD = 106.7 nM)。4A-BFA-11 通过结合聚乙二醇 (PEG) 介导的长循环 (EPR 效应) 和叶酸受体靶向作用，实现肿瘤富集。4A-BFA-11 在肿瘤部位发生酶切，释放活性有效载荷，从而实现精准作用。4A-BFA-11 在 HeLa 小鼠模型中，能高效地携带、靶向并控制 MMAE 在肿瘤组织中的释放。4A-BFA-11 可用于宫颈癌、卵巢癌和肺癌的研究。
(粉色: 靶蛋白配体；蓝色: E3 连接酶配体；黑色: 连接子)。

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4A-BFA-11

4A-BFA-11 Chemical Structure

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4A-BFA-11 相关抗体

Top Publications Citing Use of Products

查看 Folate Receptor (FR) 亚型特异性产品:

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FR-α

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

4A-BFA-11 is a folate-targeted PEG-MMAE conjugate that exhibits specific binding affinity for the folate receptor α (FR-α) (KD = 106.7 nM). 4A-BFA-11 achieves tumor enrichment by combining PEG-mediated long circulation (EPR effect) and folate receptor targeting. 4A-BFA-11 undergoes enzymatic cleavage at the tumor site to release the active payload, enabling precise action. 4A-BFA-11 sefficiently carries, targets, and controls the release of MMAE in tumor tissues in a HeLa mouse model. 4A-BFA-11 can be used for cervical cancer, ovarian cancer, and lung cancer research[1]. (Pink: Target protein ligand; Blue: E3 ligase ligand; Black: linker).

IC50 & Target[1]

FR-α

106.7 nM (Kd)

体外研究
(In Vitro)

4A-BFA-11 (72 小时) 在 HeLa、SK-OV-3 和 A549 细胞中表现出抗增殖活性，IC50 分别为 37.62、28.8 和 15.1 nM[1]。

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

4A-BFA-11 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Cmax AUC0-t AUC0-∞ Vz-F_obs CL/F
Mice[1] 1.5 mg/kg i.v. 3.04 h 6783.19 ng/mL 21168.40 ng·h/mL 21352.07 ng·h/mL 229.71 mL/kg 70.41 mL/h/kg
体内研究
(In Vivo)

4A-BFA-11 (0.4 和 0.8 mg/kg，静脉注射，每周一次，持续 2 周) 可抑制 HeLa 小鼠宫颈癌模型中的肿瘤生长[1]。

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

Animal Model: BALB/c nude mice (5-6 weeks) inoculated with HeLa graft tumors in the right axilla[1]
Dosage: 0.4 and 0.8 mg/kg
Administration: i.v., once weekly for 2 weeks
Result: Resulted in stronger antitumor effects with a tumor growth inhibition rate (T/C%) of 67.1% at 0.4 mg/kg.
Achieved pronounced antitumor effects with a T/C% of 95.9% at 0.8 mg/kg.
Showed no significant body weight loss and no significant changes in blood parameters.
Induced mild hepatitis at 0.4 mg/kg, characterized by trace inflammatory cell infiltration predominantly composed of lymphocytes and granulocytes.
Exhibited mild sinusoidal dilatation in the spleen, and the low-dose group showed slight adhesion of the white pulp.
分子量

2349.72

Formula

C113H173N23O31
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

4A-BFA-11 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

4A-BFA-11Folate Receptor (FR)folate receptor αMMAEPEG-mediated long circulationHeLaSK-OV-3A549cervical cancerovarian cancerlung cancerInhibitorinhibitorinhibit

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目录号：
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