2. Cell Cycle/DNA Damage Epigenetics
  3. PARP
  4. NMS-P118

NMS-P118是一种有效的，口服可用的，高选择性的PARP-1抑制剂，在HeLa细胞中的IC50值为0.04 μM。

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NMS-P118 Chemical Structure

NMS-P118 Chemical Structure

CAS No. : 1262417-51-5

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规格 价格 是否有货 数量
1 mg ￥429
In-stock
5 mg ￥950
In-stock
10 mg ￥1520
In-stock
25 mg ￥3040
In-stock
50 mg ￥4600
In-stock
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

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Customer Review

NMS-P118 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

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

NMS-P118 is a potent, orally available, and highly selective PARP-1 Inhibitor for cancer therapy.

IC50 & Target[1]

PARP-1

9 nM (Kd)

PARP-2

1390 nM (Kd)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
DLD-1 IC50
2 μM
Compound: 6; NMS-P118
Antiproliferative activity against human DLD-1 deficient in BRCA-2 cells measured after 7 days
Antiproliferative activity against human DLD-1 deficient in BRCA-2 cells measured after 7 days
[PMID: 34570508]
HeLa IC50
0.04 μM
Compound: 20by, NMS-P118
Inhibition of PARP1 in human HeLa cells assessed as reduction of H2O2-induced PAR formation preincubated for 30 mins followed by H2O2 addition measured after 15 mins by immunocytochemical analysis
Inhibition of PARP1 in human HeLa cells assessed as reduction of H2O2-induced PAR formation preincubated for 30 mins followed by H2O2 addition measured after 15 mins by immunocytochemical analysis
[PMID: 26222319]
MCF7 IC50
> 10 μM
Compound: 20by, NMS-P118
Cytotoxicity against human MCF7 cells assessed as inhibition of colony formation after 10 to 14 days by crystal violet staining
Cytotoxicity against human MCF7 cells assessed as inhibition of colony formation after 10 to 14 days by crystal violet staining
[PMID: 26222319]
MDA-MB-436 IC50
0.14 μM
Compound: 20by, NMS-P118
Cytotoxicity against BRCA1-deficient human MDA-MB-436 cells assessed as inhibition of colony formation after 10 to 14 days by crystal violet staining
Cytotoxicity against BRCA1-deficient human MDA-MB-436 cells assessed as inhibition of colony formation after 10 to 14 days by crystal violet staining
[PMID: 26222319]
MIA PaCa-2 IC50
> 10 μM
Compound: 20by, NMS-P118
Cytotoxicity against human MIAPaCa2 cells assessed as inhibition of colony formation after 10 to 14 days by crystal violet staining
Cytotoxicity against human MIAPaCa2 cells assessed as inhibition of colony formation after 10 to 14 days by crystal violet staining
[PMID: 26222319]
体外研究
(In Vitro)

NMS-P118 体外 的骨髓毒性低于奥拉帕尼（这是一种双重 PARP-1/-2 抑制剂）。NMS-P118 被证明是代谢稳定的，它适度抑制两个细胞色素 P450 家族成员 (CYP-2B6 IC50：8.15 μM；CYP-2D6 IC50：9.51 μM)。NMS-P118 抑制骨髓细胞增殖的能力比奥拉帕尼低 5 至 > 60 倍[1]。

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

NMS-P118 相关抗体:
体内研究
(In Vivo)

NMS-P118 是一种有效的 PARP-1 抑制剂 (KD=0.009 μM) ，比 PARP-2 (KD=1.39 μM) 选择性高 150 倍。NMS-P118 在小鼠和大鼠中具有出色的药代动力学特征和口服生物利用度。它被证明在 体内 非常有效，无论是作为 MDA-MB-436 人乳腺癌肿瘤的单一药剂，还是与替莫唑胺联合使用，在 CAPAN-1 人胰腺肿瘤中作为异种移植物在小鼠中生长。该化合物在高效剂量下具有良好的耐受性，并具有出色的 ADME 特性[1]。

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

395.42

Formula

C20H24F3N3O2
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 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 16 mg/mL (40.46 mM; 超声加热助溶; 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 2.5290 mL 12.6448 mL 25.2896 mL
5 mM 0.5058 mL 2.5290 mL 5.0579 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 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
Kinase Assay
[1]

NMS-P118 is profiled on 56 different kinases (ABL, ACK1, AKT1, ALK, AUR1, AUR2, BRK, BUB1, CDC7/DBF4, CDK2/CYCA, CHK1, CK2, EEF2K, EGFR1, ERK2, EphA2, FAK, FGFR1, FLT3, GSK3beta, Haspin, IGFR1, IKK2, IR, JAK1, JAK2, JAK3, KIT, LCK, LYN, MAPKAPK2, MELK, MET, MNK2, MPS1, MST4, NEK6, NIM1, P38alpha, PAK4, POLYDATINGFRb, POLYDATINK1, PERK, PIM1, PIM2, PKAalpha, PKCbeta, PLK1, RET, SULU1, Syk, TLK2, TRKA, TYK2, VEGFR2, ZAP70). The IC50 values are found to be >10 μM for all enzymes tested[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

NMS-P118 is dissolved in DMSO and diluted with appropriate medium before use. Cellular activity of PARP-1 inhibitors is assessed by measuring the inhibition of the hydrogen peroxide induced PAR formation in HeLa cells (ECACC). Cellular PAR levels are measured by immunocytochemistry, and quantified using an ArrayScan vTi instrument[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

The pharmacokinetic profile and the oral bioavailability of the compounds have been investigated in rat in ad hoc pharmacokinetic studies. NMS-P118 is formulated for intravenous bolus administration in 20% DMSO + 40% PEG 400 in 5% dextrose. Oral administration is performed using a NMS-P118 suspension in 0.5% methylcellulose. A single administration at the dose of 10 mg/kg for each route and a single oral administration at the dose of 100 mg/kg are given. Three male animals for each study are used[1].

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

NMS-P118 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5290 mL 12.6448 mL 25.2896 mL 63.2239 mL
5 mM 0.5058 mL 2.5290 mL 5.0579 mL 12.6448 mL
10 mM 0.2529 mL 1.2645 mL 2.5290 mL 6.3224 mL
15 mM 0.1686 mL 0.8430 mL 1.6860 mL 4.2149 mL
20 mM 0.1264 mL 0.6322 mL 1.2645 mL 3.1612 mL
25 mM 0.1012 mL 0.5058 mL 1.0116 mL 2.5290 mL
30 mM 0.0843 mL 0.4215 mL 0.8430 mL 2.1075 mL
40 mM 0.0632 mL 0.3161 mL 0.6322 mL 1.5806 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:

NMS-P1181262417-51-5PARPpoly ADP ribose polymeraseInhibitorinhibitorinhibit

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