2. Antibody-drug Conjugate/ADC Related Cytoskeleton
  3. Peptide-Drug Conjugates (PDCs) Integrin
  4. BGC0222

BGC0222 是一种新型 Irinotecan (HY-16562) 原药。BGC0222 作为一种 PEG-cRGD 偶联的 Irinotecan (HY-16562) 衍生物，可缓慢、稳定地释放 Irinotecan (HY-16562)。BGC0222 与 αVβ3 靶点结合，其 IC50 值为 4.25 μM，针对 αVβ5 的 IC50 为 58.7 μM。BGC0222 可诱导血管新生。BGC0222 在多种肿瘤中表现出良好的抗肿瘤活性。

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Custom Peptide Synthesis

BGC0222 Chemical Structure

BGC0222 Chemical Structure

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BGC0222 相关抗体

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查看 Integrin 亚型特异性产品:

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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1].

体外研究
(In Vitro)

BGC0222 (72 h) 与 Irinotecan (HY-16562) 和 NKTR-102 相比，对 HT29、MIA PaCa-2 和 MCF-7 肿瘤细胞具有更好的抗增殖活性，IC50 分别为 1.83 μM、3.95 μM 和 0.68 μM[1]。
BGC0222 (40 μM) 显示出良好的血管生成活性，血管长度达 1930 mm (CAM 血管生成试验)[1]。

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

BGC0222 相关抗体:
体内研究
(In Vivo)

BGC0222 (20-60 mg/kg，静脉注射，每 4 天或每周 1 次，共 3 次) 在 HT-29、MIA PaCa-2、NCI-H446、U-87 MG 和 MDA-MB-231 异种移植裸鼠中表现出显著的抗增殖活性，其 RTV 和 T/C 值均低于 Irinotecan[1]。
BGC0222 (30-90 mg/kg，静脉注射，每周一次，为期 28 天) 在 Sprague-Dawley 大鼠体内的安全性irinotecan 相比有所改善，最大耐受剂量 (MTD) 分别为 90 mg/kg和低于 60 mg/kg[1]。
BGC0222 (20-80 mg/kg，静脉注射，单次) 在 Sprague-Dawley 大鼠体内缓慢而稳定地释放Irinotecan[1]。

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.
分子量

26927.36

Formula

C1241H2276N64O552
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

BGC0222 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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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