1. Vps34-IN-5

Vps34-IN-5 是一种具有口服活性的 VPS34 抑制剂,对靶点的抑制率达 98%,其 IC50 被归为 B 类。Vps34-IN-5 可在癌细胞中与 EGFR 抑制剂产生相加或协同的抗增殖活性。在小鼠异种移植模型中,Vps34-IN-5 可单独口服给药,也可与 Erlotinib (HY-50896) 联合口服给药。Vps34-IN-5 可用于非小细胞肺癌的研究。

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Vps34-IN-5

Vps34-IN-5 Chemical Structure

CAS No. : 1801903-15-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Vps34-IN-5 is an orally active VPS34 inhibitor, 98% target inhibition, and an IC50 categorized as B. Vps34-IN-5 induces additive or synergistic anti-proliferative activity with EGFR inhibitors in cancer cells. Vps34-IN-5 is administered orally alone or with Erlotinib (HY-50896) in mouse xenograft models. Vps34-IN-5 can be used for the research of non-small cell lung cancer[1].

体外研究
(In Vitro)

Vps34-IN-5 (Ⅰ-299) 在 A431 细胞中与 Erlotinib (HY-50896)、Afatinib (HY-10261)、AZD9291 (HY-15772) 或 CO-1686 (HY-15729) 联合使用时表现出累加抗增殖活性,联合指数范围为 1.00 至 1.02[1]
Vps34-IN-5 在 NCI H-1650 细胞中与 afatinib、CO-1686 或 erlotinib 联用时表现出协同抗增殖活性,与 AZD9291 联用时表现出相加活性[1]
Vps34-IN-5 在 NCI-H1975 细胞中与 afatinib 或 AZD9291 联用时表现出协同抗增殖活性,与 CO-1686 联用时表现出累加活性[1]
Vps34-IN-5 在 PC9 细胞中与 erlotinib、AZD9291 或 CO-1686 联用时表现出叠加抗增殖活性,与 afatinib 联用时则表现出亚叠加活性[1]

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

体内研究
(In Vivo)

Vps34-IN-5 (0.65 mg/kg;口服;每日一次;连续 21 天) 在接种人肿瘤异种移植物的雌性裸鼠中单独使用时可抑制肿瘤生长[1]
Vps34-IN-5 (0.65 mg/kg;口服;每日一次;连续 21 天) 与 erlotinib 联用时,在携带人源肿瘤异种移植物的雌性裸鼠中可减小肿瘤体积[1]

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

Animal Model: Nude (female; inoculated subcutaneously in the flank with 2.0 × 106 tumor cells for tumor xenograft model)[1]
Dosage: 0.65 mg/kg; 0.65 mg/kg plus erlotinib (50/mg/kg)
Administration: p.o.; daily; 21 days
Result: Inhibited tumor growth when used alone.
Reduced tumor volume when used in combination with erlotinib.
分子量

502.92

Formula

C22H17ClF2N6O2S

CAS 号
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

Vps34-IN-5 相关分类

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  • 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.

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产品名称:
Vps34-IN-5
目录号:
HY-182378
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