BGC0222 is a novel Irinotecan original drug. As a PEG-cRGD-coupled Irinotecan derivative, BGC0222 can release Irinotecan slowly and stably. BGC0222 binds to the αVβ3 target with an IC50 value of 4.25 μM, and the IC50 for αVβ5 is 58.7 μM. BGC0222 can induce angiogenesis. BGC0222 shows good anti-tumor activity in a variety of tumors.

Physicochemical Properties

Molecular Formula	C1241H2276N64O552
Molecular Weight	26927.36
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	BGC0222 (72 h) exhibits superior antiproliferative activity against HT29, MIA PaCa-2, and MCF-7 tumor cells compared to Irinotecan and NKTR-102, with IC50 values of 1.83 μM, 3.95 μM, and 0.68 μM, respectively[1]. BGC0222 (40 μM) showed good angiogenic activity, with vessel length reaching 1930 mm (CAM angiogenesis assay)[1].
ln Vivo	BGC0222 (20-60 mg/kg, intravenous injection, every 4 days or once a week for 3 times) showed significant antiproliferative activity in HT-29, MIA PaCa-2, NCI-H446, U-87 MG and MDA-MB-231 xenograft nude mice, with lower RTV and T/C values than Irinotecan[1]. BGC0222 (30-90 mg/kg, intravenously, once a week for 28 days) showed improved safety compared with irinotecan in Sprague-Dawley rats, with maximum tolerated doses (MTDs) of 90 mg/kg and less than 60 mg/kg, respectively[1]. BGC0222 (20-80 mg/kg, single intravenous injection) releases irinotecan slowly and steadily in Sprague-Dawley rats[1].
Animal Protocol	Animal/Disease Models: 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] Doses: 20 mg/kg (MIA PaCa-2, NCI-H446, MDA-MB-231); 40 mg/kg (HT-29); 60 mg/kg (U-87 MG) Route of 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 Experimental Results: 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.
References	[1]. Design, synthesis and pharmacological evaluation of a novel PEG-cRGD-conjugated irinotecan derivative as potential antitumor agent. Eur J Med Chem. 2018 Oct 5, 158:82-90.

Solubility Data

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	0.0371 mL	0.1857 mL	0.3714 mL
	5 mM	0.0074 mL	0.0371 mL	0.0743 mL
	10 mM	0.0037 mL	0.0186 mL	0.0371 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.