BGC0222

Cat. No.: HY-P10783: FAQs
Data Sheet Handling Instructions Technical Support

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 α_Vβ₃ with IC₅₀ values of 4.25 μM (α_Vβ₃) and 58.7 μM (α_Vβ₅). BGC0222 possesses the property of inducing neovascularization. BGC0222 exhibits good antiproliferation activity in many tumors.

For research use only. We do not sell to patients.

BGC0222 Chemical Structure

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•Related Small Molecules:

•Related Proteins:

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αvβ1 αvβ3 αvβ5 αvβ6 αvβ8 α5β1 α1β1 α2β1 α4β1 α9β1 αIIbβ3 α4β7 αLβ2

Biological Activity
Purity & Documentation
References
Customer Review

Description

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 (20-60 mg/kg, i.v., every 4 days or once a week, 3 times) exhibits remarkable antiproliferation activity in the 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 that of Irinotecan (HY-16562). BGC0222 (30-90 mg/kg, i.v., once weekly for a 28-day period) improves safety profile relative to irinotecanin in Sprague-Dawley rats, with the maximum tolerated dose (MTD) of 90 mg/kg and less than 60 mg/kg, respectively^[1].
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.

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]
Dosage:	20 mg/kg (MIA PaCa-2, NCI-H446, MDA-MB-231); 40 mg/kg (HT-29); 60 mg/kg (U-87 MG)
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
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.

Molecular Weight

26927.36

Formula

C₁₂₄₁H₂₂₇₆N₆₄O₅₅₂

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Huang YQ, et al. 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. [Content Brief]

BGC0222 Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BGC0222BGC 0222BGC-0222Peptide-Drug Conjugates (PDCs)IntegrinHT29MIA PaCa-2MCF-7NCI-H446AntiproliferationBalb/c.Inhibitorinhibitorinhibit

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