Faridoxorubicin
Faridoxorubicin (AVA-6000) is a FAP-activated chemotherapeutic prodrug. Faridoxorubicin undergoes selective hydrolysis by FAP, while it is resistant to cleavage by related mammalian peptidases and members of the DASH subfamily. Faridoxorubicin acts as a tumor growth inhibitor, reducing tumor volume and prolonging survival in in vivo models and PDX models with high FAP expression. Faridoxorubicin can be used in the research of osteosarcoma and sarcoma.
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- No. CAS: 1841402-73-0
- Fòrmula: C41H44N4O14
- Peso molecular:816.81
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-29 | EC50 |
210 μM
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Cell growth inhibition against HT29 cells treated with AVA6000 alone, measured via in vitro cytotoxicity assay.
Cell growth inhibition against HT29 cells treated with AVA6000 alone, measured via in vitro cytotoxicity assay.
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AACR2022_1815.pdf |
| BXPC-3 | EC50 |
250 μM
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Cell growth inhibition against BxPC-3 cells treated with AVA6000 alone, measured via in vitro cytotoxicity assay.
Cell growth inhibition against BxPC-3 cells treated with AVA6000 alone, measured via in vitro cytotoxicity assay.
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AACR2022_1815.pdf |
| MCF7 | EC50 |
160 μM
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Cell growth inhibition against MCF-7 cells treated with AVA6000 alone, measured via in vitro cytotoxicity assay.
Cell growth inhibition against MCF-7 cells treated with AVA6000 alone, measured via in vitro cytotoxicity assay.
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AACR2022_1815.pdf |
| MDA-MB-231 | EC50 |
160 μM
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Cell growth inhibition against MDA-MB-231 cells treated with AVA6000 alone, measured via in vitro cytotoxicity assay.
Cell growth inhibition against MDA-MB-231 cells treated with AVA6000 alone, measured via in vitro cytotoxicity assay.
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AACR2022_1815.pdf |
| OVCAR-3 | EC50 |
250 μM
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Cell growth inhibition against OVCAR-3 cells treated with AVA6000 alone, measured via in vitro cytotoxicity assay.
Cell growth inhibition against OVCAR-3 cells treated with AVA6000 alone, measured via in vitro cytotoxicity assay.
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AACR2022_1815.pdf |
| SK-OV-3 | EC50 |
12 μM
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Cell growth inhibition against SK-OV-3 cells treated with AVA6000 alone, measured via in vitro cytotoxicity assay.
Cell growth inhibition against SK-OV-3 cells treated with AVA6000 alone, measured via in vitro cytotoxicity assay.
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AACR2022_1815.pdf |
| NCI-H460 | EC50 |
1.1 μM
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Cell growth inhibition against NCI-H460 cells treated with AVA6000 alone, measured via in vitro cytotoxicity assay.
Cell growth inhibition against NCI-H460 cells treated with AVA6000 alone, measured via in vitro cytotoxicity assay.
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AACR2022_1815.pdf |
| A549 | EC50 |
43 μM
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Cell growth inhibition against A549 cells treated with AVA6000 alone, measured via in vitro cytotoxicity assay.
Cell growth inhibition against A549 cells treated with AVA6000 alone, measured via in vitro cytotoxicity assay.
|
AACR2022_1815.pdf |
In Vitro
Faridoxorubicin (1 μM; 30 min) is selectively hydrolyzed by recombinant FAP to release Doxorubicin (HY-15142A)[1].
Faridoxorubicin exhibits only extremely low intrinsic cytotoxicity in cancer cells, but its cytotoxicity is significantly enhanced after activation by FAP, either via FAP on the surface of HEK-mFAP cells or exogenously added soluble FAP[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | Note | Tmax | Cmax | T1/2 | AUC0-last | AUC0-∞ | CL | Vd |
|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 9 mg/kg | i.v. | Male | 0.033 h | 27800 ng/mL | 4.59 h | 4410 ng·h/mL | 4420 ng·h/mL | 2040 mL/h/kg | 13500 mL/kg |
| Dog[1] | 2 mg/kg | i.v. | / | 0.033 h | 4883 ng/mL | 0.458 h | 345 ng·h/mL | 347 ng·h/mL | 6780 mL/h/kg | 4520 mL/kg |
| Rat[1] | 9 mg/kg | i.v. | Female | 0.033 h | 20600 ng/mL | 6.89 h | 2960 ng·h/mL | 2970 ng·h/mL | 3030 mL/h/kg | 30100 mL/kg |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1841402-73-0
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Peso molecular 816.81
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Fòrmula C41H44N4O14
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SMILES
OC1=C(C(C2=CC=CC(OC)=C2C3=O)=O)C3=C(O)C4=C1C[C@](C(CO)=O)(O)C[C@@H]4O[C@H]5C[C@@H]([C@@H]([C@@H](O5)C)O)NC([C@H]6N(CCC6)C([C@@H](C)NC(C7=CC=NC=C7)=O)=O)=O
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Synonyms
AVA-6000
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Faridoxorubicin Related Classifications
HY-177083 Related Classifications
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