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United States

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製品番号: HY-P10783

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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 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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

分子式: C₁₂₄₁H₂₂₇₆N₆₄O₅₅₂
分子量:26927.36

保管条件:

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

BGC0222 構造式

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

One-Stop Platform：From Independent R&D to Pilot-Scale Production

生物活性

製品説明

Integrin アイソフォーム固有の製品をすべて表示 :

体外実験

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.

体内実験

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.

化学情報

分子量 26927.36
分子式 C₁₂₄₁H₂₂₇₆N₆₄O₅₅₂
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (262 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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]

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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.

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100 mg

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