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.
- Formula: C113H173N23O31
- Molecular Weight:2349.72
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
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. Further protocols information, click here.
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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (5-6 weeks) inoculated with HeLa graft tumors in the right axilla[1]
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Dosage:0.4 and 0.8 mg/kg
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Administration:i.v., once weekly for 2 weeks
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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.
Chemical Information
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Molecular Weight 2349.72
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Formula C113H173N23O31
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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How to Choose the Right Model Animal
Choosing the right model animal is a validity-driven decision in which the species, strain, sex, age, genetic background, disease-induction method, outcome measures, and welfare burden must match the scientific question rather than laboratory tradition or convenience. A model should be selected by judging face validity, construct validity, and predictive validity: whether it resembles the human phenotype, whether it reproduces relevant mechanisms, and whether results are likely to predict human biology or treatment response. Animal studies often fail to translate because of species differences, weak disease resemblance, poor experimental design, inadequate reporting, publication bias, and underuse of randomization, blinding, and sample-size justification. Unresolved questions include how to rank competing models objectively, how much human-disease complexity must be reproduced for a given objective, and when non-animal systems such as organoids, ex vivo tissue, or computational models
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)