1. Cell Cycle/DNA Damage Apoptosis
  2. Wee1 Apoptosis
  3. WEE1-IN-7

WEE1-IN-7 (compound 12h) 是一种有效的具有口服活性的 WEE1 抑制剂,其IC50值为 2.1 nM。WEE1-IN-7 诱导细胞凋亡 (apoptosis) 和细胞周期停滞于 S 期。WEE1-IN-7 具有抗肿瘤活性。

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WEE1-IN-7 Chemical Structure

WEE1-IN-7 Chemical Structure

CAS No. : 2924006-98-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

WEE1-IN-7 (compound 12h) is a potent and orally activeWEE1 inhibitor with an IC50 value of 2.1 nM. WEE1-IN-7 induces apoptosis and cell cycle arrest at the S phase. WEE1-IN-7 shows antitumor activity[1].

IC50 & Target

IC50: 2.1 nM (WEE1)[1]

体外研究
(In Vitro)

WEE1-IN-7 (compound 12h) 抑制细胞活力,对 A427 和 Lovo 细胞的 IC50 值分别为 84 和 82 nM[1]
WEE1-IN-7 (0-800 nM; 48 h) 以剂量依赖性方式诱导细胞凋亡和细胞周期停滞在 S 期[1]

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

Apoptosis Analysis[1]

Cell Line: A427 cells
Concentration: 200, 400, 800 nM
Incubation Time: 48 h
Result: Significantly increased the percentage of both early and late apoptotic cells in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: A427 cells
Concentration: 0, 50, 100, 200, 400 nM
Incubation Time: 48 h
Result: Induced cell cycle arrest at the S phase with the the percentage of cells in the S phase of 37.4%, 46.7%, 48.5%, 59.1%, and 59.1% at 0, 50, 100, 200, and 400 nM, respectively.
体内研究
(In Vivo)

WEE1-IN-7 (60 mg/kg; p.o.; daily for 27 days) 在 Lovo CDX 异种移植小鼠模型中表现出抗肿瘤活性,肿瘤生长抑制率 (TGI) 为 88%[1]
药代动力学分析[1].

Admin. AUC (h·ng/mL) T1/2 (h) Vd (L/kg) CL (L/h/kg) Cmax F (%)
intravenous (1 mg/kg) 118 1.06 11.3 8.20 - -
intragastric (60 mg/kg) 4342 5.94 - - 498 61.64

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

Animal Model: Female C57 mice (Lovo CDX xenograft mice model)[1]
Dosage: 60 mg/kg
Administration: P.o.; daily for 27 days
Result: Showed antitumor activity with the tumor growth inhibition (TGI) of 88%.
分子量

520.59

Formula

C28H28N10O

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
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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:
WEE1-IN-7
目录号:
HY-163697
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