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

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.

For research use only. We do not sell to patients.

4A-BFA-11

4A-BFA-11 Chemical Structure

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Description

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].

IC50 & Target[1]

FR-α

106.7 nM (Kd)

In Vitro

4A-BFA-11 (72 h) exhibits antiproliferation activity in HeLa, SK-OV-3, and A549 cells, with IC50s of 37.62, 28.8, and 15.1 nM, respectively[1].

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

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
In Vivo

4A-BFA-11 (0.4 and 0.8 mg/kg, i.v., once weekly for 2 weeks) inhibits tumor growth in a HeLa mouse cervical cancer model[1].

MedChemExpress (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.
Molecular Weight

2349.72

Formula

C113H173N23O31

SMILES

O=C(NCCOCCOCC(NCCOCCOCCOCCNC(CC[C@@H](C(O)=O)NC(C1=CC=C(C=C1)NCC2=NC(C(NC(N)=N3)=O)=C3N=C2)=O)=O)=O)COCCOCCNC([C@@H](CCC(N[C@@H](C(C)C)C(N[C@H](CCCNC(N)=O)C(N(C)C4=CC=C(C=C4)COC(N([C@H](C(N[C@H](C(N(C)[C@@H]([C@H](CC)C)[C@@H](CC(N5[C@@H](CCC5)[C@@H]([C@H](C(N[C@@H]([C@H](C6=CC=CC=C6)O)C)=O)C)OC)=O)OC)=O)C(C)C)=O)C(C)C)C)=O)=O)=O)=O)NC(CCCCCN7C(CCC7=O)=O)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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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.

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Product Name:
4A-BFA-11
Cat. No.:
HY-180557
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