Stenoparib是一种口服生物可用的强效小分子 PARP1 和 PARP2 抑制剂,能够增强放疗和化疗的效果,在 BRCA 缺陷的肿瘤中具有强大的单药抗癌活性。
HazMat Fee + There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
| Type | HazMat fee for 500 gram (Estimated) |
| Excepted Quantity | USD 0.00 |
| Limited Quantity | USD 15-60 |
| Inaccessible (Haz class 6.1), Domestic | USD 80+ |
| Inaccessible (Haz class 6.1), International | USD 150+ |
| Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
| Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |


| 规格 | 价格 | 会员价 | 库存 | 数量 | |||
|---|---|---|---|---|---|---|---|
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| 产品名称 | PARP ↓ ↑ | PARP1 ↓ ↑ | PARP2 ↓ ↑ | PARP3 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| PJ34 HCl |
++
PARP, EC50: 20 nM |
99%+ | |||||||||||||||||
| Rucaparib phosphate |
++++
PARP, Ki: 1.4 nM |
99%+ | |||||||||||||||||
| 3-Aminobenzamide |
++
PARP, IC50: <50 nM |
98% | |||||||||||||||||
| AZD-2461 | ✔ | 99%+ | |||||||||||||||||
| BGP-15 | ✔ | 99%+ | |||||||||||||||||
| NU1025 |
+
PARP, IC50: 400 nM |
98% | |||||||||||||||||
| Benzamide |
+
PARP, IC50: 3.3 μM |
98% | |||||||||||||||||
| Picolinamide |
+
PARP, IC50: 95 μM |
98% | |||||||||||||||||
| AG14361 |
+++
PARP1, Ki: <5 nM |
98+% | |||||||||||||||||
| Iniparib | ✔ | 98% | |||||||||||||||||
| Talazoparib |
++++
PARP1, IC50: 0.57 nM |
99%+ | |||||||||||||||||
| NMS-P118 |
++
PARP1, Kd: 0.009 μM |
97% | |||||||||||||||||
| UPF 1069 |
+
PARP1, IC50: 8.0 μM |
++
PARP2, IC50: 0.3 μM |
98% | ||||||||||||||||
| A-966492 |
++++
PARP1, Ki: 1 nM PARP1, EC50: 1 nM |
+++
PARP2, Ki: 1.5 nM |
99%+ | ||||||||||||||||
| Veliparib |
++
PARP1, Ki: 5.2 nM |
+++
PARP2, Ki: 2.9 nM |
98% | ||||||||||||||||
| Niraparib tosylate |
+++
PARP1, IC50: 3.8 nM |
+++
PARP2, IC50: 2.1 nM |
99%+ | ||||||||||||||||
| Stenoparib |
++++
PARP1, IC50: 1 nM |
++++
PARP2, IC50: 1.2 nM |
98% | ||||||||||||||||
| Olaparib |
+++
PARP1, IC50: 5 nM |
++++
PARP2, IC50: 1 nM |
98% | ||||||||||||||||
| Niraparib |
+++
PARP1, IC50: 3.8 nM |
+++
PARP2, IC50: 2.1 nM |
98% | ||||||||||||||||
| ME0328 |
+
PARP1, IC50: 6.3 μM |
+
PARP3, IC50: 0.89 μM |
99%+ | ||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 靶点 |
|
| 描述 | E7449 is an orally bioavailable, potent, small molecule inhibitor of PARP1 and PARP2 and enhances the efficacy of radiotherapy and chemotherapy and has potent single agent anticancer activity in BRCA-deficient tumors. |
| Concentration | Treated Time | Description | References | |
| DLD-1 cells | 10 μmol/L | 24 h | To evaluate the effect of E7449 on Wnt signaling, results showed increased axin2 protein levels. | Oncotarget. 2015 Dec 1;6(38):41307-23. |
| SW480 cells | 10 μmol/L | 24 h | To evaluate the effect of E7449 on Wnt signaling, results showed increased axin2 protein levels and decreased β-catenin levels. | Oncotarget. 2015 Dec 1;6(38):41307-23. |
| DT40 cells | 0.1-10 μmol/L | 30 min | To evaluate the role of E7449 in DNA damage repair, results showed increased PARP1 binding to chromatin. | Oncotarget. 2015 Dec 1;6(38):41307-23. |
| LLC-MK2 rhesus macaque kidney cells | 30 μM | 120 hours | Evaluate the inhibitory effect of Stenoparib on HCoV-NL63, showing a 69.3% reduction in plaquing efficiency and 95.8% reduction in viral copy number | mBio. 2021 Jan 19;12(1):e03495-20. |
| Calu-3 human lung adenocarcinoma cells | 60 μM | 120 hours | Evaluate the inhibitory effect of Stenoparib on SARS-CoV-2, showing nearly complete inhibition of plaque formation (94.0%) | mBio. 2021 Jan 19;12(1):e03495-20. |
| Vero E6 monkey kidney cells | 30 μM | 48 hours | Evaluate the inhibitory effect of Stenoparib on SARS-CoV-2, showing a significant 63.2% reduction in viral load | mBio. 2021 Jan 19;12(1):e03495-20. |
| A549 cells | 10 mol/L | 48 hours | E7449 significantly downregulated TNKS expression, inhibited proliferation, migration, and invasion of A549 cells, and induced early apoptosis. | J Cell Mol Med. 2024 Jun;28(12):e18467. |
| A549L6 cells | 5.753 µM (IC50) | 96 hours | Evaluate the inhibitory effect of E7449 on proliferation and migration of A549L6 cells | Cancers (Basel). 2025 Feb 6;17(3):559. |
| Administration | Dosage | Frequency | Description | References | ||
| Mice | B16-F10 isograft model | Orally | 10, 30, 100 mg/kg | Once daily for 7 days | To evaluate the antitumor effect of E7449 in combination with TMZ, results showed significantly enhanced tumor growth inhibition. | Oncotarget. 2015 Dec 1;6(38):41307-23. |
| BALB/c nude mice | Subcutaneous xenograft model with A549 cells | Gavage | 100 mg/kg | Once daily for 14 days | E7449 significantly inhibited the growth of subcutaneous lung adenocarcinoma tumors and induced apoptosis by attenuating the Wnt signaling pathway. | J Cell Mol Med. 2024 Jun;28(12):e18467. |
| BALB/c nude mice | LUAD bone metastasis model | Oral | 40 mg/kg | Once daily for 21 days | Evaluate the inhibitory effect of E7449 on bone metastasis | Cancers (Basel). 2025 Feb 6;17(3):559. |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
3.15mL 0.63mL 0.32mL |
15.76mL 3.15mL 1.58mL |
31.51mL 6.30mL 3.15mL |
|
| CAS号 | 1140964-99-3 |
| 分子式 | C18H15N5O |
| 分子量 | 317.34 |
| SMILES Code | O=C1NNC2=C3C1=CC=CC3=NC(CN4CC5=C(C=CC=C5)C4)=N2 |
| MDL No. | MFCD28167842 |
| 别名 | E7449; 2X-121; MGI25036 |
| 运输 | 蓝冰 |
| InChI Key | JLFSBHQQXIAQEC-UHFFFAOYSA-N |
| Pubchem ID | 135565981 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, 2-8°C |
| 溶解方案 |
DMSO: 5 mg/mL(15.76 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
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