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Art. -Nr.: HY-177083

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Faridoxorubicin

Name: Faridoxorubicin
Brand: MedChemExpress
SKU: HY-177083
Availability: PreOrder

(Synonyms: AVA-6000)

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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 1841402-73-0
Formel: C₄₁H₄₄N₄O₁₄
Molecular Weight:816.81

Speicherung:

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

Data Sheet (299 KB)

Faridoxorubicin Chemical Structure

CAS. Nr.: 1841402-73-0

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
- Clinical Trial
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
HT-29	EC50	210 μM	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.	AACR2022_1815.pdf
BXPC-3	EC50	250 μM	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.	AACR2022_1815.pdf
MCF7	EC50	160 μM	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.	AACR2022_1815.pdf
MDA-MB-231	EC50	160 μM	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.	AACR2022_1815.pdf
OVCAR-3	EC50	250 μM	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.	AACR2022_1815.pdf
SK-OV-3	EC50	12 μM	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.	AACR2022_1815.pdf
NCI-H460	EC50	1.1 μM	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.	AACR2022_1815.pdf
A549	EC50	43 μM	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

Anti-cancerOthers

Anti-cancer

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].

Others

Faridoxorubicin (1 μM; 30 min) is selectively hydrolyzed by recombinant FAP to release Doxorubicin (HY-15142A)^[1].

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

Parmacokinetics

Species	Dose	Route	Note	T_max	C_max	T_1/2	AUC_0-last	AUC_0-∞	CL	V_d
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

Anti-cancer

Faridoxorubicin (12 mg/kg; intravenous injection; once weekly; 4 total administrations) induces 67% tumor growth inhibition in heavily pretreated, FAP-expressing human sarcoma PDX models^[1].

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

Related Protocols :

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991			2011-05	PHASE1

Chemical Information

CAS. Nr. 1841402-73-0
Molecular Weight 816.81
Formel C₄₁H₄₄N₄O₁₄
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
Synonyms

AVA-6000
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (299 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. McLaughlin, Fiona, et al. "AVA6000, a novel precision medicine, targeted to the tumor microenvironment via fibroblast activation protein (FAP) mediated cleavage." Cancer Res 82.12_Supplement (2022): 1815.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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