2. PROTAC PI3K/Akt/mTOR
  3. PROTACs PI3K
  4. PROTAC PI3Kα degrader-1

PROTAC PI3Kα degrader-1 是一种 PI3Kα 的 PROTAC 降解剂 (DC50 = 0.08 μM)，其对 PI3Kα 的降解作用表现出显著的选择性，相较于 PI3Kβ、PI3Kγ 和PI3Kδ 亚型具有明显优势。PROTAC PI3Kα degrader-1 以时间和浓度依赖性方式有效降解 PI3Kα，并有效抑制 Ser473 位点 AKT 的磷酸化。 PROTAC PI3Kα degrader-1 在 HGC-27 和 DOHH2 异种移植模型中显示出显著的体内抗癌功效。(粉色：PI3Kα 配体：(HY-174798)，蓝色：E3 连接酶 CRBN 配体 (HY-10984)，黑色：连接子，E3 连接酶配体-接头偶联物：HY-W940885)。

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PROTAC PI3Kα degrader-1

PROTAC PI3Kα degrader-1 Chemical Structure

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PROTAC PI3Kα degrader-1 相关抗体

Top Publications Citing Use of Products

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查看 PI3K 亚型特异性产品:

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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

PROTAC PI3Kα degrader-1 is a PI3Kα PROTAC degrader (DC50 = 0.08 μM), demonstrating good selectivity for PI3Kα degradation over PI3Kβ, PI3Kγ, and PI3Kδ. PROTAC PI3Kα degrader-1 effectively degrades PI3Kα in a time- and concentration-dependent, over PI3Kβ, PI3Ky and PI3Kδ, and potently inhibited the phosphorylation of AKT at the Ser473site. PROTAC PI3Kα degrader-1 shows significant in vivo anticancer efficacy in HGC-27 and DOHH2 xenograft models. (Pink: PI3Kα ligand : (HY-174798), Blue: E3 ligase CRBN Ligand (HY-10984), Black: Linker, E3 ligase ligand-linker conjugate (HY-W940885))[1].

IC50 & Target[1]

Cereblon

 

PI3Kα

62 nM (IC50)

PI3Kβ

293.94 nM (IC50)

PI3Kγ

>10000 nM (IC50)

PI3Kδ

42.10 (IC50)

体外研究
(In Vitro)

PROTAC PI3Kα degrader-1 (Compound 12) (1 μM) 在 T47D 乳腺癌细胞中对 79 种激酶显示出微弱活性 (< 20%)，对 PIK3CA 表现出强效抑制(＞ 95%)[1]。

PROTAC PI3Kα degrader-1 (0.1-10 μM) 在 T47D 乳腺癌细胞中对 PI3Kα 的降解表现出相较于 PI3Kβ、PI3Kγ 和 PI3Kδ 的良好选择性[1]。

PROTAC PI3Kα degrader-1 在多种癌细胞系中对 PI3Kα 的降解表现出优异的选择性，对 T47D 细胞的IC50 值为0.35 μM，对 MDA-MB-453 细胞的 IC50 值为 1.64 μM，对 HGC-27 细胞的 IC50 值为1.45 μM，对 AGS 细胞的 IC50 值为0.37 μM ，对 LNCaP 细胞的 IC50 值为3.38 μM，对 PC3 细胞的 IC50 值为 1.48 μM，对 Pfeiffer 细胞的 IC50 值为 0.69 μM[1]。

PROTAC PI3Kα degrader-1 (0.0032-10 μM, 0-24 h) 在 T47D 和 HGC-27 细胞中以浓度和时间依赖的方式降解 PI3Kα[1]。

PROTAC PI3Kα degrader-1 (1 μM, 20 h) 在 T47D 细胞中通过 CRBN 招募经由泛素-蛋白酶体途径降解 PI3Kα[1]。

PROTAC PI3Kα degrader-1 (0.1-10 μM, 24 h) 在 T47D 细胞中以浓度依赖的方式诱导G2/M 期细胞周期阻滞[1]。

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

PROTAC PI3Kα degrader-1 相关抗体:

Western Blot Analysis[1]

Cell Line: T47D cells
Concentration: 1 μM
Incubation Time: 20h with/without MG132 (HY-13259) (1 μM)
Result: Reduced the level of PI3Kα, while the addition of MG132 restored PI3Kα levels.

RT-PCR[1]

Cell Line: T47D cells
Concentration: 1 μM
Incubation Time: 24 h
Result: Did not decrease the mRNA levels of PIK3CA.

Western Blot Analysis[1]

Cell Line: T47D cells
Concentration: 1 μM
Incubation Time: 8 h after Thalidomide (HY-14658) (10 μM) preincubated 1h and then incubated in fresh medium for an additional 48 hours.
Result: Degraded PI3Kα but preincubation with thalidomide (10 μM, 1 h) reduced this degradation.
Restored PI3Kα expression to normal levels 48 h after an 8h treatment followed by incubation in fresh medium.
体内研究
(In Vivo)

PROTAC PI3Kα degrader-1 (Compound 12) (2 μM, 0-60 min) 在包括小鼠、大鼠、狗、猴和人的所有测试物种中显示出优异的血浆稳定性[1]。

PROTAC PI3Kα degrader-1 (2 μM, 0-60 min) 在各物种中表现出中到高的清除率，半衰期 (t1/2) 分别为小鼠 22.6 min、大鼠 45.7 min、狗 67.6 min、猴 32.5 min 和人 34.7 min，且高度依赖 NADPH[1]。

PROTAC PI3Kα degrader-1 (30-60 mg/kg，腹腔注射，每天注射连续 15 天) 在 HGC-27 异种移植模型中显示出显著的抗癌效果[1]。

PROTAC PI3Kα degrader-1 (30 mg/kg，腹腔注射，每天注射连续 21 天) 在 DOHH2 异种移植模型中显示出显著的抗癌效果[1]。

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

Animal Model: Male BALB/c nude mice (20-22 g) bearing HGC-27 xenografts[1]
Dosage: 30, 60 mg/kg
Administration: i.p. daily for 14 days
Result: Showed tumor growth rates (TGI) of 38.3% at 30 mg/kg and 56.8% at 60 mg/kg.
Induced dose-dependent degradation of PI3Kα.
Showed no significant changes in body weight.
Animal Model: Male BALB/c nude mice (20-22 g) bearing DOHH2 xenografts[1]
Dosage: 30 mg/kg
Administration: i.p. daily for 21 days
Result: Demonstrated a strong efficacy with a tumor growth inhibition (TGI) rate of 61.8%, which is more effective than Ibrutinib (HY-10997) administered orally at a dose of 25 mg/kg and Idelalisib (HY-13026) administered orally at a dose of 10 mg/kg.
Showed no significant body weight loss.
分子量

897.99

Formula

C46H49F2N7O8S
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

PROTAC PI3Kα degrader-1 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • 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:

PROTAC PI3Kα degrader-1PROTACsPI3KPhosphoinositide 3-kinaseCancerHGC-27DOHH2PI3KαInhibitorinhibitorinhibit

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