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

PROTAC PI3Kα/δ degrader-1 是一种具有口服活性的 PI3Kα/δ PROTAC 降解剂，PI3Kα 的 IC50 为 0.34 nM，PI3Kδ 的 IC50 为 1.85 nM。PROTAC PI3Kα/δ degrader-1 可抑制癌细胞的增殖、迁移、诱导 G1 期细胞周期阻滞和 PI3Kα 降解。PROTAC PI3Kα/δ degrader-1 可抑制乳腺癌异种移植小鼠模型中的肿瘤生长。PROTAC PI3Kα/δ degrader-1 可用于乳腺癌的研究。
(粉色: 靶蛋白配体；蓝色: Ligands for E3 Ligase 配体 (HY-A0003)；黑色: 连接子)。

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PROTAC PI3Kα/δ degrader-1

PROTAC PI3Kα/δ degrader-1 Chemical Structure

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PROTAC PI3Kα/δ degrader-1 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC PI3Kα/δ degrader-1 is an orally active PI3Kα/δ PROTAC degrader, with an IC50 of 0.34 nM for PI3Kα and 1.85 nM for PI3Kδ. PROTAC PI3Kα/δ degrader-1 inhibits the proliferation and migration of cancer cells, induces G1-phase cell cycle arrest and PI3Kα degradation. PROTAC PI3Kα/δ degrader-1 suppresses tumor growth in breast cancer xenograft mouse models. PROTAC PI3Kα/δ degrader-1 can be used for the research of breast cancer[1]. (Pink: Target protein ligand; Blue: Ligands for E3 Ligase ligand (HY-A0003); Black: linker).

IC50 & Target[1]

PI3Kα

0.34 nM (IC50)

PI3Kβ

7.02 nM (IC50)

PI3Kδ

1.85 nM (IC50)

PI3Kγ

1.95 nM (IC50)

VHL

 

体外研究
(In Vitro)

PROTAC PI3Kα/δ degrader-1 (Compound D5) 抑制 PI3Kα、PI3Kβ、PI3Kδ、PI3Kγ、酶活性，IC50 分别为 0.34、7.02、1.85、1.95 nM[1]。
PROTAC PI3Kα/δ degrader-1 (72 h) 可强效抑制 T47D 细胞 (IC50 = 0.06 nM) 和 MCF7 细胞 (IC50 = 2.65 nM) 的增殖[1]。
PROTAC PI3Kα/δ degrader-1 (0.002-100 nM; 8 h) 可在 T47D 细胞中诱导 PI3Kα 发生强效的、剂量依赖性降解，其 DC50 为 0.05 nM[1]。
PROTAC PI3Kα/δ degrader-1 (1-10 nM; 2 weeks) 可抑制 MCF7 乳腺癌细胞的集落形成[1]。
PROTAC PI3Kα/δ degrader-1 (10-50 nM; 12-24 h) 可通过划痕愈合实验检测抑制 MCF7 乳腺癌细胞的迁移[1]。
PROTAC PI3Kα/δ degrader-1 (0.1-10 nM; 24 h) 可在 T47D 乳腺癌细胞中诱导剂量依赖性 G1 期细胞周期阻滞，在 10 nM 时阻滞作用达到峰值[1]。

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

PROTAC PI3Kα/δ degrader-1 相关抗体:

Western Blot Analysis[1]

Cell Line: T47D cells
Concentration: 0.002-100 nM
Incubation Time: 8 h
Result: Induced dose-dependent degradation of PI3Kα in T47D cells, with a DC50 of 0.05 nM.

Cell Migration Assay[1]

Cell Line: MCF7 breast cancer cells
Concentration: 10, 50 nM
Incubation Time: 12-24 h
Result: Significantly inhibited MCF7 cell migration into the wound area.

Cell Cycle Analysis[1]

Cell Line: T47D breast cancer cells
Concentration: 0.1, 1, 10 nM
Incubation Time: 24 h
Result: Induced G1 phase cell cycle arrest in a dose-dependent manner, with 10 nM increasing G1 phase cells to 80.1%.
体内研究
(In Vivo)

PROTAC PI3Kα/δ degrader-1 (20-40 mg/kg；腹腔注射/口服；每日 1 次；21 天) 可显著抑制 BALB/c 裸鼠体内 T47D、MCF7 乳腺癌异种移植物的生长[1]。

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

Animal Model: BALB/c nude mice (female, tumor-bearing, n=5 per group)[1]
Dosage: 20 mg/kg; 40 mg/kg
Administration: i.p.; once daily; 21 days; p.o.; once daily; 21 days
Result: Significantly reduced tumor volume compared to the control group.
Showed no significant body weight loss in any treated group.
Significantly inhibited the growth of MCF7 breast cancer xenografts.
分子量

877.00

Formula

C45H56N12O7
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/δ 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 *
= × ×

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/δ degrader-1PROTACsPI3KPhosphoinositide 3-kinasePI3Kα/δ PROTAC degraderT47D cellsMCF7 cellsBALB/c nude micebreast cancerInhibitorinhibitorinhibit

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