2. PI3K/Akt/mTOR
  3. PI3K
  4. PI3Kα-IN-31

PI3Kα-IN-31 是一种具有口服活性的选择性 PI3Kα 抑制剂。PI3Kα-IN-31 相较于野生型 PI3Kα，对突变型 PI3Kα 表现出显著偏好性。PI3Kα-IN-31 可在 PI3Kα 突变型癌细胞中发挥抗增殖作用。PI3Kα-IN-31 可抑制异种移植模型中的肿瘤生长。PI3Kα-IN-31 可用于乳腺癌的研究。

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PI3Kα-IN-31

PI3Kα-IN-31 Chemical Structure

CAS No. : 3115133-30-4

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PI3Kα-IN-31 相关抗体

Top Publications Citing Use of Products

查看 PI3K 亚型特异性产品:

查看所有亚型
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PI3Kα-IN-31 is an orally active and selective PI3Kα inhibitor. PI3Kα-IN-31 shows potent preference for mutant PI3Kα over wild-type PI3Kα. PI3Kα-IN-31 exerts antiproliferative effects in PI3Kα-mutant cancer cells. PI3Kα-IN-31 suppresses tumor growth in xenograft models. PI3Kα-IN-31 can be used for the research of breast cancer[1].

IC50 & Target[1]

PI3Kα

87.35 nM (IC50)

p110α-H1047R

14.2 nM (IC50)

p110α-E542K

24.58 nM (IC50)

p110α-E545K

31.88 nM (IC50)

体外研究
(In Vitro)

PI3Kα-IN-31 (compound B10) (0-1000 nM; 30 min pre-incubation, 1 h reaction) 可选择性抑制纯化的 PI3KαH1047R、PI3KαE542K 和 PI3KαE545K 突变酶，其 IC50 值分别为 14.2 nM、24.58 nM 和 31.88 nM；而对野生型 PI3Kα 的抑制活性较弱，IC50 为 87.35 nM[1]。
PI3Kα-IN-31 (0-10 μM; 96 h) 可强效抑制携带 PI3Kα 突变的 T-47D 和 MCF-7 乳腺癌细胞的增殖，其 IC50 值分别为 9.7 nM 和 18.6 nM，而对携带野生型 PI3Kα 的 SKBR3 细胞无显著抑制作用[1]。

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

PI3Kα-IN-31 相关抗体:
体内研究
(In Vivo)

PI3Kα-IN-31 (compound B10) (25-50 mg/kg；口服；每日一次；连续 20 天) 可剂量依赖性地抑制 NOD-SCID 小鼠体内 MCF-7 乳腺癌异种移植物的生长，TGI 分别达到 86.29% 和 97.17%，且具有良好的体内耐受性[1]。

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

Animal Model: NOD-SCID (female, 4-6 weeks old, subcutaneous inoculation of MCF-7 cells)[1]
Dosage: 25 mg/kg; 50 mg/kg
Administration: p.o.; daily; 20 days
Result: Reached average tumor volumes of 333.6 mm3 and 210.5 mm3 on day 12 at doses of 25 mg/kg and 50 mg/kg, respectively.
Achieved tumor growth inhibition (TGI) rates of 86.29% and 97.17% at doses of 25 mg/kg and 50 mg/kg, respectively.
Showed no significant body weight loss or other adverse reactions during the study period.
分子量

631.94

Formula

C29H19ClF5N5O4
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

PI3Kα-IN-31 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:

PI3Kα-IN-313115133-30-4PI3KPhosphoinositide 3-kinaseT-47DE542KPI3Kα-mutant cancer cellswild-type PI3KαH1047Rbreast cancerMCF-7xenograft modelsE545KPI3KαInhibitorinhibitorinhibit

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目录号：
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