2. Cell Cycle/DNA Damage Epigenetics
  3. PARP
  4. PARP1-IN-40

PARP1-IN-40 是一种具有高度选择性的具有口服活性的 PARP1 抑制剂 (IC50: PARP1 为 0.19 nM，PARP2 为 26 nM)。PARP1-IN-40 通过抑制 PARP1导致 DNA 损伤累积，杀死肿瘤细胞。PARP1-IN-40 对 BRCA 突变的 MDA-MB-436 细胞具有较高的抗肿瘤活性。PARP1-IN-40 可以与化疗联合用于癌症的相关研究。

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PARP1-IN-40 Chemical Structure

PARP1-IN-40 Chemical Structure

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PARP1-IN-40 相关抗体

Top Publications Citing Use of Products

查看 PARP 亚型特异性产品:

查看所有亚型
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PARP1-IN-40 is a highly selectively and orally active PARP1 inhibitor (IC50: 0.19 nM for PARP1, 26 nM for PARP2). PARP1-IN-40 kills tumor cells by inhibiting PARP1, leading to accumulation of DNA damage. PARP1-IN-40 has high antitumor activity against BRCA mutant MDA-MB-436 cells. PARP1-IN-40 can be used in combination with chemotherapy for cancer-related research[1].

体外研究
(In Vitro)

PARP1-IN-40 (Compound (S)-G9) (1-100 nM, 3 days) 阻滞 MDA-MB-436 细胞周期于 G2/M 期抑制增殖[1]。

PARP1-IN-40 (0.1-1000 nM, 3 days) 在 MDA-MB-436 细胞中诱导 DNA 损伤，双链断裂[1]。

PARP1-IN-40 (0.1-10000 nM, 1 h) 在 A549 细胞的 PARP1 基因敲除细胞中几乎无活性 (IC50 > 9.8 μM)，证明其作用完全依赖于 PARP1，且其对 PARP2 的抑制活性极弱，从而避免了传统 PARPi 的毒性风险[1]。

PARP1-IN-40 (0.1-10000 nM, 1 h) 高效捕获 PARP1-DNA 复合物 (EC50 = 1.9 nM)，而捕获 PARP2 需超千倍浓度，是 PARP1 选择性捕获剂[1]。

PARP1-IN-40 (0.1-20000 nM, 10 days) 可选择性杀死 BRCA 突变细胞，证实其合成致死机制依赖于同源重组缺陷[1]。


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

PARP1-IN-40 相关抗体:

Cell Cycle Analysis[1]

Cell Line: MDA-MB-436 cells
Concentration: 1 nM, 10 nM, 100 nM
Incubation Time: 3 days
Result: Reduced the number of cells in S phase and significantly increased the number of cells in G2/M phase in a dose-dependent manner.

Cell Proliferation Assay[1]

Cell Line: MDA-MB-436 cells, DLD-1 BRCA2-KO cells, DLD-1 WT cells
Concentration: 0.1 nM, 1 nM, 10 nM, 100 nM (MDA-MB-436 cells, DLD-1 BRCA2-KO cells); 2.5 μM, 5 μM, 10 μM, 20 μM (DLD-1 WT cells)
Incubation Time: 10 days
Result: Completely inhibited clone formation in BRCA1 mutant (MDA-MB-436) and BRCA2 null (DLD-1 KO) cells at low concentrations, and showed no toxicity to BRCA wild-type cells (DLD-1 WT) even at high concentrations.

Immunofluorescence[1]

Cell Line: MDA-MB-436 cells
Concentration: 0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM
Incubation Time: 3 days
Result: Significantly increased the number of γH2AX foci.

Western Blot Analysis[1]

Cell Line: MDA-MB-436 cells
Concentration: 0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM
Incubation Time: 3 days
Result: Increased the expression of γH2AX.
药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Mice 1 mg/kg i.v. Tmax 0.008 h
Mice 1 mg/kg p.o. AUC0-t 2.4E5 ng·h/mL
Mice 10 mg/kg i.v. Tmax 0.08 h
Mice 10 mg/kg p.o. Tmax 2 h
Mice 3 mg/kg i.v. Tmax 0.08 h
Mice 3 mg/kg p.o. AUC0-t 9.3E5 ng·h/mL
Rat 2.5 mg/kg i.v. AUC0-t 7.0E4 ng·h/mL
Rat 2.5 mg/kg p.o. Tmax 5 h
Mice 1 mg/kg i.v. Cmax 1.2E4 ng/mL
Mice 1 mg/kg p.o. Cmax 6.6E3 ng/mL
Mice 10 mg/kg i.v. Cmax 4.9E4 ng/mL
Mice 10 mg/kg p.o. Cmax 3.8E4 ng/mL
Mice 3 mg/kg i.v. Cmax 1.8E4 ng/mL
Mice 3 mg/kg p.o. Cmax 2.0E4 ng/mL
Rat 2.5 mg/kg i.v. Cmax 5.3E3 ng/mL
Rat 2.5 mg/kg p.o. Cmax 3.2E3 ng/mL
Mice 1 mg/kg i.v. AUC0-t 2.4E5 ng·h/mL
Mice 1 mg/kg p.o. Tmax 3.01 h
Mice 10 mg/kg i.v. AUC0-t 1.5E6 ng·h/mL
Mice 10 mg/kg p.o. AUC0-t 1.5E6 ng·h/mL
Mice 3 mg/kg i.v. AUC0-t 7.3E5 ng·h/mL
Mice 3 mg/kg p.o. Tmax 2 h
Rat 2.5 mg/kg i.v. Tmax 0.08 h
Rat 2.5 mg/kg p.o. AUC0-t 6.2E4 ng·h/mL
体内研究
(In Vivo)

PARP1-IN-40 (Compound (S)-G9) (0.3-3 mg/kg, p.o, 连续27天) 在 MDA-MB-231 异种移植小鼠模型中强效抑制 BRCA 突变肿瘤生长，无显著毒性[1]。

PARP1-IN-40 (1-3 mg/kg, p.o, 连续14天) 在 HCT116 异种移植小鼠模型中与化疗协同增效[1]。

PARP1-IN-40 (30-300 mg/kg, p.o, 给药一次; 30-100 mg/kg, p.o, 连续14天) 在 BALB/C 裸鼠中安全性高[1]。

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

Animal Model: MDA-MB-231 xenograft model established in nude mice[1]
Dosage: 0.3 mg/kg, 1 mg/kg, 3 mg/kg
Administration: Oral administration (p.o.), at the corresponding doses for 27 days
Result: Had TGI of 80 % at a dose of 0.3 mg/kg and 94 % at 3 mg/kg, with stable mouse body weight.
Blocked DNA repair in tumor tissues by selectively inhibiting PARP1, leading to the accumulation of γH2AX-mediated DNA damage, which in turn downregulated Ki67 to inhibit proliferation and drive anti-tumor efficacy.
Animal Model: HCT116 xenograft model established in nude mice[1]
Dosage: 1 mg/kg or 3mg/kg + liposomal Irinotecan (HY-16562) (2 mg/kg)
Administration: PARP1-IN-40: Oral administration (p.o.), at the corresponding doses for 14 days; liposomal Irinotecan: Intravenous injection (i.v.), twice weekly for 14 days.
Result: Had a TGI of 80 % at 1 mg/kg combined with chemotherapy and 85 % at 3 mg/kg.
Animal Model: Famale and male BALB/C nude mice[1]
Dosage: 30 mg/kg, 100 mg/kg, 300 mg/kg
Administration: Oral administration (p.o.) at 30 mg/kg and 100 mg/kg for 14 days; Oral administration (p.o.) at 30 mg/kg, 100 mg/kg and 300mg/kg once dose
Result: Did not cause death or significant weight changes in mice, and the histology of the heart, liver, spleen, lung, and kidney was normal.
Had no significant organ toxicity even at doses far higher than the therapeutic dose, and had excellent oral safety.
分子量

445.49

Formula

C25H24FN5O2
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

PARP1-IN-40 相关分类

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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:

PARP1-IN-40PARPpoly ADP ribose polymeraseBRCAPARP1MDA-MB-436 cellsHCT116 cellsDLD-1 BRCA2-KO cellsA549 WT cellsInhibitorinhibitorinhibit

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