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

NMS-P118是一種有效的，口服可用的，高選擇性的PARP-1抑制劑，在HeLa細(xì)胞中的IC50值為0.04 μM。

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NMS-P118 Chemical Structure

NMS-P118 Chemical Structure

CAS No. : 1262417-51-5

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     可免費申領(lǐng)三個不同產(chǎn)品的試用裝。

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥826
In-stock
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 現(xiàn)貨 詢價
200 mg   詢價  
500 mg   詢價  

* Please select Quantity before adding items.

Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 2 篇科研文獻(xiàn)

  • 生物活性

  • 實驗參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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)

細(xì)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]
體外研究
(In Vitro)

NMS-P118 體外 的骨髓毒性低于奧拉帕尼（這是一種雙重 PARP-1/-2 抑制劑）。NMS-P118 被證明是代謝穩(wěn)定的，它適度抑制兩個細(xì)胞色素 P450 家族成員 (CYP-2B6 IC50：8.15 μM；CYP-2D6 IC50：9.51 μM)。NMS-P118 抑制骨髓細(xì)胞增殖的能力比奧拉帕尼低 5 至 > 60 倍[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

NMS-P118 是一種有效的 PARP-1 抑制劑 (KD=0.009 μM) ，比 PARP-2 (KD=1.39 μM) 選擇性高 150 倍。NMS-P118 在小鼠和大鼠中具有出色的藥代動力學(xué)特征和口服生物利用度。它被證明在 體內(nèi) 非常有效，無論是作為 MDA-MB-436 人乳腺癌腫瘤的單一藥劑，還是與替莫唑胺聯(lián)合使用，在 CAPAN-1 人胰腺腫瘤中作為異種移植物在小鼠中生長。該化合物在高效劑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 號
性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實驗： 

DMSO 中的溶解度 : 16 mg/mL (40.46 mM; 超聲加熱助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)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
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
參考文獻(xiàn)
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.
參考文獻(xiàn)

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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.

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產(chǎn)品名稱：
NMS-P118
目錄號：
HY-18954
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