BGC0222
BGC0222 is a novel prodrug of Irinotecan (HY-16562). BGC0222, as a PEG-cRGD-conjugated Irinotecan (HY-16562) derivative, could slowly and steadily release Irinotecan (HY-16562). BGC0222 binds to αVβ3 with IC50 values of 4.25 μM (αVβ3) and 58.7 μM (αVβ5). BGC0222 possesses the property of inducing neovascularization. BGC0222 exhibits good antiproliferation activity in many tumors.
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- Fòrmula: C1241H2276N64O552
- Peso molecular:26927.36
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Actividad biológica
Descripciòn
In Vitro
BGC0222 (72 h) exhibits better antiproliferation activity than Irinotecan (HY-16562) and NKTR-102 against HT29, MIA PaCa-2 and MCF-7 tumor cell lines, with IC50 of 1.83 μM, 3.95 μM and 0.68 μM, respectively[1].
BGC0222 (40 μM) shows good angiogenesis activity, with the length of blood vessels of 1930 mm (CAM angiogenesis assay)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
BGC0222 (20-80 mg/kg, i.v., single) slowly and steadily release irinotecan in Sprague-Dawley rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HT-29, MIA PaCa-2, NCI-H446, U-87 MG and MDA-MB-231 xenograft female Balb/c nude mice (HT-29, 4 × 106; MIA PaCa-2, 5 × 106; NCI-H446, 8 × 106; U-87 MG,4 × 106; MDA-MB-231, 3 × 106)[1]
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Dosage:20 mg/kg (MIA PaCa-2, NCI-H446, MDA-MB-231); 40 mg/kg (HT-29); 60 mg/kg (U-87 MG)
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Administration:Intravenous injection (i.v.), every 4 days (HT-29 and MDA-MB-231) or once a week (MIA PaCa-2, NCI-H446 and U-87 MG), 3 times
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Result:Exhibited remarkable antiproliferation activity in the HT-29, MIA PaCa-2, NCI-H446, U-87 MG and MDA-MB-231 xenograft nude mice.
Exhibited that T/C values of BGC0222 for days 12, 15, 18, 22, 25, 29 and 32 were determined to be 100%, 88.8%, 57.0%, 27.6%, 16.9%, 9.87% and 9.21%, while that of irinotecan were found to be 100%, 103%, 93.1%, 75.1%, 68.8%, 60.6%, 71.1% in the HT-29 xenograft nude mice, respectively.
Showed that the RTV values of BGC0222 were much lower than that of irinotecan and NKTR-102 when the average tumor size reached approximately 100–300 mm3 (after day 12) in the HT-29 xenograft nude mice.
Chemical Information
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Peso molecular 26927.36
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Fòrmula C1241H2276N64O552
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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)
BGC0222 Related Classifications
HY-P10783 Related Classifications
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