2. Cell Cycle/DNA Damage Epigenetics
  3. PARP
  4. PARP1-IN-34

PARP1-IN-34 (compound 30) 是一种PARP1 的选择性抑制剂，IC50 为 0.32 nM。PARP1-IN-34 是一种亚纳摩尔 PARP1 抑制剂，对 PARP2 的选择性为 1000 倍，IC50 为 326 nM。PARP1-IN-34 具有抗癌活性。

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PARP1-IN-34 Chemical Structure

PARP1-IN-34 Chemical Structure

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PARP1-IN-34 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-34 (compound 30) is a selective PARP1 inhibitor with an IC50 of 0.32 nM. PARP1-IN-34 is a subnanomolar PARP1 inhibitor with >1000-fold selectivity against PARP2 with an IC50 of 326 nM. PARP1-IN-34 shows antitumor efficacy[1].

IC50 & Target

PARP1

0.32 nM (IC50)

PARP2

326 nM (IC50)

体外研究
(In Vitro)

PARP1-IN-34 显示在 60，120，180 min 时捕获 PARP1 的 EC50 分别为 34.7，65.9，102.7 nM[1]。
PARP1-IN-34 显示出对 PARP2 的捕获非常弱，EC50 为 9882 nM [1]。
PARP1-IN-34 (180min) 形成了比 Palacaparib (AZD-9574) (HY-145804) 更紧密的 PARP1-DNA 捕获。 PARP1-IN-34 (10 nM, 72 h) 刺激 MDA-MB-436 细胞中的 DNA 双链断裂。 PARP1-IN-34 (10 nM, 72 h) 可增加 MDA-MB-436 细胞中 γH2AX 的水平，并比 AZD9574 对细胞造成更严重的 DNA 损伤[1]。
PARP1-IN-34 在 BRCA WT 细胞 (CAL-148，22RV1 和 PC3 细胞) 和 293T 正常细胞(IC50 > 10,000 nM) 中抗增殖活性很小，而在 BRCA 突变的 MDA-MB-436 细胞中，其 IC50 为 2.6 nM，这表明其对细胞的抗增殖活性是 PARP1 抑制依赖性的[1]。
与其他 PARP (包括 PARP2，PARP3，PARP5A，PARP5B，PARP6，PARP7，PARP12，PARP14 和 PARP15) 相比，PARP1-IN-34 是一种高度选择性 PARP1 抑制剂[1]。

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

PARP1-IN-34 相关抗体:

Western Blot Analysis

Cell Line: MDA-MB-436 cells
Concentration: 10 nM
Incubation Time: 72 h
Result: Increased the levels of γH2AX at 10 nM in MDA-MB-436 cells and causes more significant DNA damage in cells than AZD9574
体内研究
(In Vivo)

PARP1-IN-34 (0.2-0.6 mg/kg, p.o., daily, 35 天) 在 MDA-MB-436 小鼠异种移植模型中，以剂量依赖性方式诱导肿瘤缩小[1]。
PARP1-IN-34 (10 mg/kg, p.o., daily, 35 天) 在 SUM149P T 异种移植模型中，与 Carboplatin (HY-17393) 具有协同作用[1]。
PARP1-IN-34 (5, 25 mg/kg, p.o., daily, 14 天) 对网织红细胞减少的影响最小[1]。
PARP1-IN-34 在小鼠，大鼠和狗中的药代动力学。

与其他PARP抑制剂相比，PARP1-IN-34的治疗指数。
property mouse rat dog
plasma protein unbound fraction 0.012 0.067 0.022
t1/2 (h) 3.2 5.1 9.2
V ss(L/kg) 0.34 1.42 0.36
CLp(mL/min/kg) 2.0 4.9 0.58
AUC(0-t)(ng・h r/mL) po 45688 13622 15024
F(%) 132.4 93.1 67.3

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

Compound Olaparib AZD5305 AZD9574 PARP1-IN-34
Potency PARP1 IC50(nM)
PARP2 IC50(nM)
PARP 1/2 fold selectivity		 0.95
0.34
0.39
 0.46
10
22		 0.87
672
772
 0.32
326
1019
In vivo efficacy in MDA-MB-436 Dose of tumor regression ≥50%
AUC (ng/ml hr)
Unbound % in mice
Free - drug AUC (ng/ml hr)		 100 mg/kg
31426
29.3%
9208		 0.1 mg/kg
4043
2%
81		 2 mg/kg
9776
4%
391		 0.6 mg/kg
1039
1.2%
12.5
Hematox in rat Dose of RET > 50%↓
AUC (ng/ml hr)
Unbound % in rat
Free - drug AUC (ng/ml hr)		 <100 mg/kg
55803
26.6%
14844		 < 1 mg/kg
7505
2%
150.1		 >100 mg/kg
308365
9.7%
29911		 > 25 mg/kg
133541
6.7%
8947
Therapeutic index Fold of Free - drug AUC <1.61 < 1.71 >76.5 >715
Animal Model: Female Balb/c athymic nude mice (Vital River) (6-8 weeks) were subcutaneously implanted with 1 × 107 MDA-MB-436 cells in 0.2 mL Matrigel solution in the right flank[1] .
Dosage: 0.2, 0.6 mg/kg
Administration: p.o., daily, 35 days
Result: At 0.6 mg/kg QD induced tumor shrinkage by 65.7%, which was stronger than the efficacy of AZD9574 at 0.6 mg/kg QD (38.1% shrinkage) and that of AZD5305 at 0.03 mg/kg QD (24.4% shrinkage).
Induced minimal changes in animal body weight.
Animal Model: Female Balb/c athymic nude mice (Vital River) (6−8 weeks) were subcutaneously implanted with 1 × 107 SUM149PT cells in 0.2 mL Matrigel solution in the right flank.[1] .
Dosage: 10 mg/kg
Administration: p.o., daily, 35 days
Result: In combination with weekly 37.5 mg/kg carboplatin demonstrated great improvement of the antitumor effect compared to carboplatin monotherapy (94.7% TGI vs 69.7% TGI).
Induced no significant body weight loss during the study.
Animal Model: Female Balb/c athymic nude mice (Vital River) (6−8 weeks) were subcutaneously implanted with 1 × 107 SUM149PT cells in 0.2 mL Matrigel solution in the right flank.[1] .
Dosage: 5, 25 mg/kg
Administration: p.o., daily, 14days
Result: Had minimal impact on RET(reduction of the reticulocyte).
Induced no significant body weight loss during the study.
分子量

433.51

Formula

C23H27N7O2
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-34 相关分类

  • 摩尔计算器

  • 稀释计算器

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

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× = ×
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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:

PARP1-IN-34PARPpoly ADP ribose polymerasecancerhematologicalDNA damageInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-170432
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