2. PI3K/Akt/mTOR
  3. PI3K Akt
  4. PI3Kα-IN-32

PI3Kα-IN-32 (Compound 11f) 是一种选择性的、具有口服活性的 PI3Kα 抑制剂，对 PI3KαH1047R 的 IC50 为 26.3 nM。PI3Kα-IN-32 抑制 AKT 磷酸化。PI3Kα-IN-32 对乳腺癌具有抗癌活性。PI3Kα-IN-32 可用于 HR+/HER2- 乳腺癌的研究。

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PI3Kα-IN-32

PI3Kα-IN-32 Chemical Structure

CAS No. : 3057582-20-1

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PI3Kα-IN-32 相关抗体

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PI3Kα-IN-32 (Compound 11f) is a selective, orally active PI3Kα inhibitor, with an IC50 of 26.3 nM against PI3KαH1047R. PI3Kα-IN-32 inhibits AKT phosphorylation. PI3Kα-IN-32 exhibits anticancer activity against breast cancer. PI3Kα-IN-32 can be used in the research of HR+/HER2- breast cancer[1].

IC50 & Target[1]

PI3Kα-H1047R

26.3 nM (IC50)

PI3Kα

94.6 nM (IC50)

体外研究
(In Vitro)

PI3Kα-IN-32 可强效且选择性地抑制 PI3KαH1047R 突变体酶活性，其 IC50 为 26.3 nM[1]。
PI3Kα-IN-32 (10 μM max; 144 h) 可强效抑制 T47D HR+/HER2- 乳腺癌细胞的增殖，其 IC50 为 88.8 nM，对表达野生型 PI3Kα 的 SK-BR-3 乳腺癌细胞的选择性是前者的 14.7 倍[1]。
PI3Kα-IN-32 可抑制 T47D HR+/HER2- 乳腺癌细胞中的 AKT 磷酸化，其 IC50 为 29.0 nM，且对表达野生型 PI3Kα 的 SK-BR-3 乳腺癌细胞的选择性是前者的 5.8 倍[1]。
PI3Kα-IN-32 (10 μM) 对 PI3Kα 具有高度选择性，对 PI3Kδ 和 PIK3C3 仅表现出微弱活性，且对其他 108 种受试激酶无显著活性[1]。

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

PI3Kα-IN-32 相关抗体:

Cell Proliferation Assay[1]

Cell Line: T47D HR+/HER2- breast cancer cells, SK-BR-3 wild-type PI3Kα breast cancer cells
Concentration: 10 μM (max, serial 4-fold dilutions)
Incubation Time: 144 h
Result: Inhibited T47D cell proliferation with an IC50 of 88.8 nM.
Inhibited SK-BR-3 cell proliferation with an IC50 of 1307.5 nM, giving a T47D/SK-BR-3 selectivity ratio of 14.7.
药代动力学
(Parmacokinetics)
Species Dose Route Cmax AUC T1/2
Mice[1] 100 mg/kg p.o. 8830 ng/mL 61400 ng·h/mL 4.13 h
Rat[1] 100 mg/kg p.o. 25948 ng/mL 284091 ng·h/mL 5.04 h
体内研究
(In Vivo)

PI3Kα-IN-32 (50-150 mg/kg；口服；每日 1 次；21 天) 在 T47D 异种移植小鼠中展现出强效的、剂量依赖性抗肿瘤活性[1]。

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

Animal Model: BALB/c Nude (female, 6-8 weeks old, subcutaneous inoculation of T47D cells with 17β-estradiol tablet implantation)[1]
Dosage: 50 mg/kg; 100 mg/kg; 150 mg/kg
Administration: p.o.; QD; 21 days
Result: Produced 77% tumor growth inhibition (TGI = 0.77) at 50 mg/kg.
Attained complete tumor regression at 100 mg/kg (TGI = 1.06) and 150 mg/kg (TGI = 1.19).
Showed no significant body weight loss at all tested dosages.
Caused no significant changes in plasma insulin levels at 4 h and 24 h post-dose.
Decreased tumor p-AKT (Ser473) levels by over 90% within 4 h of oral administration.
Confirmed dose-dependent inhibition of AKT phosphorylation in tumor tissue after treatment.
分子量

487.45

Formula

C20H18F5N5O2S
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-32 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

PI3Kα-IN-323057582-20-1PI3KAktPhosphoinositide 3-kinasePKBProtein kinase BT47D HR+/HER2- breast cancer cellsPIK3CA H1047R mutant PI3KαT47D xenograft miceHEK 293 cellshERG channelsSD ratsSK-BR-3 breast cancer cellsCYP enzymesAKT phosphorylationHR+/HER2- breast cancerInhibitorinhibitorinhibit

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产品名称：
PI3Kα-IN-32
目录号：
HY-183285
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