2. Cell Cycle/DNA Damage Epigenetics
  3. PARP
  4. Simmiparib

Simmiparib 是一种高效且具有口服活性的 PARP1 和 PARP2 抑制剂，IC50 分别为 1.75 nM 和 0.22 nM。Simmiparib 对 PARP1/2 的抑制作用强于其母体化合物 Olaparib (HY-10162)。在同源重组修复 (HR) 缺陷细胞中，Simmiparib 诱导 DNA 双链断裂 (DSB) 积累和 G2/M 阻滞，从而诱导细胞凋亡 (apoptosis)。Simmiparib 在细胞和裸鼠移植瘤模型中都表现出显著的抗癌活性。

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Simmiparib Chemical Structure

Simmiparib Chemical Structure

CAS No. : 1551355-46-4

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规格 价格 是否有货 数量
1 mg ￥1590
In-stock
5 mg ￥3500
In-stock
10 mg ￥5800
In-stock
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100 mg   询价  

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Customer Review

Simmiparib 相关抗体

Top Publications Citing Use of Products

查看 PARP 亚型特异性产品:

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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

Simmiparib is a highly potent and orally active PARP1 and PARP2 inhibitor with IC50 values of 1.75 nM and 0.22 nM, respectively. Simmiparib has more potent PARP1/2 inhibition than its parent Olaparib (HY-10162). Simmiparib induces DNA double-strand breaks (DSB) accumulation and G2/M arrest in homologous recombination repair (HR)-deficient cells, thereby inducing apoptosis. Simmiparib exhibits remarkable anticancer activities in cells and nude mice bearing xenografts[1].

IC50 & Target[1]

PARP1

0.74 nM (IC50)

PARP2

0.22 nM (IC50)

体外研究
(In Vitro)

Simmiparib (0-10 μM; 3 days) exhibits anti-proliferative activity against various cancer cells[1].
Simmiparib (0-10 μM; 48 h) induces typical G2/M arrest in Capan-1 cells[1].
Simmiparib (0.1-2 μM; 24 h) induces apoptosis in MDA-MB-436 and V-C8 (BRCA2-/-) cells, and increases dose-dependently the levels of γH2AX[1].
Simmiparib (1-10 μM; 48 h or 72 h) increases the phosphorylation levels of Chk1 and Chk2 and the protein levels of p-Cyclin B1 (S147), Cyclin B1, p-CDK1 (Y15) and CDK1[1].

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

Simmiparib 相关抗体:

Cell Proliferation Assay[1]

Cell Line: Various cancer cells harboring deficient BRCA1, BRCA2, PTEN and EWS-FLI1
Concentration: 0-10 μM
Incubation Time: 3 days
Result: Exhibited anti-proliferative activity against MDA-MB-436 (BRCA1-/-), RD-ES (EWS-FLI1), DoTc2-4510 (BRCA2-/-), Capan-1 (BRCA2-/-) and U251 (PTEN-/-) with IC50s of 0.2 nM, 4.6 nM, 20 nM, 21 nM and 36 nM, respectively.

Cell Cycle Analysis[1]

Cell Line: Capan-1 cells
Concentration: 0, 1, 3 and 10 μM
Incubation Time: 48 h
Result: Induced typical G2/M arrest in a concentration-dependent manner.

Apoptosis Analysis[1]

Cell Line: MDA-MB-436
Concentration: 0.1 and 1 μM
Incubation Time: 24 h
Result: Led to 39.64% and 42.98% apoptosis at 0.1 and 1 μM, respectively.
Increased dose-dependently the levels of γH2AX.

Apoptosis Analysis[1]

Cell Line: V-C8 (BRCA2-/-)
Concentration: 0.5 and 2 μM
Incubation Time: 24 h
Result: Caused more than 57% apoptosis.

Western Blot Analysis[1]

Cell Line: Capan-1
Concentration: 1 and 10 μM
Incubation Time: 48 h or 72 h
Result: Increased the phosphorylation levels of Chk1 and Chk2 but did not change the levels of the corresponding total proteins.
Increased the protein levels of p-Cyclin B1 (S147), Cyclin B1, p-CDK1 (Y15) and CDK1.
体内研究
(In Vivo)

Simmiparib (2, 4 and 8 mg/kg; p.o.; qd, for 14 days) inhibits the growth of tumor in V-C8 (BRCA2-/-) and MDA-MB-436 (BRCA2-/-) xenograft mice models[1].
Simmiparib (10 and 50 mg/kg; p.o.; qd, for 42 days) inhibits the growth of BRCA1-mutated breast cancer in xenograft mice model[1].

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

Animal Model: Female BALB/cA nude mice (Subcutaneously injected with BRCA2-/- V-C8 cells and BRCA2-/- MDA-MB-436 cells)[1]
Dosage: 2, 4 and 8 mg/kg
Administration: p.o.; qd, for 14 days
Result: Apparently inhibited the growth of the V-C8 tumor with an inhibition rate of 74.53% at 8 mg/kg.
Suppressed the growth of the BRCA1-deficient MDA-MB-436 xenografts in a dose-dependent manner with its average inhibition rates of 64.93, 82.98 and 85.79% at 2, 4 and 8 mg/kg.
Did not cause significant loss of body weight.
Animal Model: Female BALB/cA nude mice (Subcutaneously injected with cancer cells derived from BRCA1-mutated BR-05-0028 breast cancer tissue)[1]
Dosage: 10 and 50 mg/kg
Administration: p.o.; qd, for 42 days
Result: Elicited dose-dependent growth inhibition with the inhibition rate of 76.73% and 93.82% at 10 mg/kg and 50 mg/kg, respectively.
Clinical Trial
分子量

486.42

Formula

C23H18F4N6O2
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (205.58 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0558 mL 10.2792 mL 20.5584 mL
5 mM 0.4112 mL 2.0558 mL 4.1117 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

Simmiparib 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0558 mL 10.2792 mL 20.5584 mL 51.3959 mL
5 mM 0.4112 mL 2.0558 mL 4.1117 mL 10.2792 mL
10 mM 0.2056 mL 1.0279 mL 2.0558 mL 5.1396 mL
15 mM 0.1371 mL 0.6853 mL 1.3706 mL 3.4264 mL
20 mM 0.1028 mL 0.5140 mL 1.0279 mL 2.5698 mL
25 mM 0.0822 mL 0.4112 mL 0.8223 mL 2.0558 mL
30 mM 0.0685 mL 0.3426 mL 0.6853 mL 1.7132 mL
40 mM 0.0514 mL 0.2570 mL 0.5140 mL 1.2849 mL
50 mM 0.0411 mL 0.2056 mL 0.4112 mL 1.0279 mL
60 mM 0.0343 mL 0.1713 mL 0.3426 mL 0.8566 mL
80 mM 0.0257 mL 0.1285 mL 0.2570 mL 0.6424 mL
100 mM 0.0206 mL 0.1028 mL 0.2056 mL 0.5140 mL
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:

Simmiparib1551355-46-4PARPpoly ADP ribose polymeraseanticancerantitumorV-C8MDA-MB-436Capan-1PTENEWS-FLI1BRCA1BRCA2Inhibitorinhibitorinhibit

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