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.
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- Formule: C113H173N23O31
- Masse moléculaire:2349.72
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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.
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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Masse moléculaire 2349.72
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
4A-BFA-11 Related Classifications
HY-180557 Related Classifications
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