上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。
Onvansertib (Synonyms: NMS-1286937; NMS-P937) 纯度: 99.32%
nMS-1286937 是一种有效、高选择性、可口服的 PLK1 抑制剂,IC50 值为 2 nM。
Onvansertib Chemical Structure
CAS No. : 1034616-18-6
规格 | 价格 | 是否有货 | 数量 |
---|---|---|---|
Free Sample (0.1-0.5 mg) | Apply now | ||
10 mM * 1 mL in DMSO | ¥762 | In-stock | |
5 mg | ¥650 | In-stock | |
10 mg | ¥1000 | In-stock | |
50 mg | ¥2600 | In-stock | |
100 mg | ¥4900 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
* Please select Quantity before adding items.
Onvansertib 相关产品
•相关化合物库:
- Drug Repurposing Compound Library Plus
- Clinical Compound Library Plus
- Bioactive Compound Library Plus
- Apoptosis Compound Library
- Cell Cycle/DNA Damage Compound Library
- Kinase Inhibitor Library
- Anti-Cancer Compound Library
- Clinical Compound Library
- Anti-Aging Compound Library
- Drug Repurposing Compound Library
- Orally Active Compound Library
- Anti-Blood Cancer Compound Library
- Targeted Diversity Library
生物活性 |
NMS-1286937 is a potent, selective and orally available PLK1 inhibitor, with an IC50 of 2 nM. |
||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
IC50 & Target[1] |
|
||||||||||||||||
体外研究 (In Vitro) |
NMS-1286937 is a potent, selective and orally available PLK1 inhibitor, with IC50 of 2 nM. NMS-1286937 also shows inhibitory activities against FLT3, MELK, and CK2, with IC50s of 510, 744, and 826 nM, respectively[1]. NMS-P937 possesses a pure ATP competitive mechanism with a reversible dissociation and no time dependency. NMS-P937 (10 μM) is selective with a marginal activity of 48% and 40% inhibition on PLK2 and PLK3, respectively. NMS-P937 shows antiproliferative activity against a panel of 137 cell lines, with IC50 values of below 100 nM for 60 of 137 cell lines and higher than 1 μM for only 9 of 137 cell lines[2]. NMS-P937 shows cytotoxic activity against AmL-NS8 cells with IC50 of 36 nM[3]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
||||||||||||||||
体内研究 (In Vivo) |
NMS-1286937 (45 mg/kg, i.v.) shows a good tumor growth inhibition with acceptable and reversible body weight loss in CD1 nu/nu mice xenografted with human HCT116 colon adenocarcinoma cells. NMS-1286937 (60 mg/kg, p.o.) also inhibits the growth of tumor on HCT116 xenograft model[1]. NMS-P937 (45 mg/kg, i.v.or 60 mg/kg, p.o) inhibits tumor growth to a comparable degree (TGI, 83% and 79% intravenously and orally, respectively) in HCT116-bearing mice. The combination of NMS-P937 (120 mg/kg given for 4 cycles of 2 consecutive days with 10-day rest) and cytarabine (75 mg/kg for 4 cycles of 5 consecutive days with 7-day rest) in the disseminated leukemia model AmL-PS is well tolerated and clearly showed increased mice survival[2]. NMS-P937 (60 mg/kg bid os per day over 2 days with a 5 day rest) shows good efficacy compared to standard therapies, with a significant increase in median survival time (MST) in the established disease setting[3]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
||||||||||||||||
Clinical Trial |
|
||||||||||||||||
分子量 |
532.52 |
||||||||||||||||
Formula |
C24H27F3N8O3 |
||||||||||||||||
CAS 号 |
1034616-18-6 |
||||||||||||||||
运输条件 |
Room temperature in continental US; may vary elsewhere. |
||||||||||||||||
储存方式 |
|
||||||||||||||||
溶解性数据 |
In Vitro:
DMSO : 21 mg/mL (39.44 mM; Need ultrasonic and warming) 配制储备液
*
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。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
|
||||||||||||||||
参考文献 |
|
Kinase Assay [1] |
The inhibitory activity of putative kinase inhibitors and the potency of selected compounds are determined using a trans-phosphorylation assay. Specific peptide or protein substrates are trans-phosphorylated by their specific serine-threonine or tyrosine kinase, in the presence of ATP traced with 33P-γ-ATP, at optimized buffer and cofactors conditions. At the end of the phosphorylation reaction, more than 98% unlabeled ATP and radioactive ATP is captured by adding an excess of the ion exchange dowex resin; the resin then settles down to the bottom of the reaction plate by gravity. Supernatant, containing the phosphorylated substrate, is subsequently withdrawn and transferred into a counting plate, followed by evaluation by b-counting. Inhibitory potency evaluation for all the tested kinases is performed at 25°C using a 60 min end-point assay where the concentrations of ATP and substrates are kept equal to 2 × αKm and saturated (>5 × αKm), respectively. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
---|---|
Cell Assay [2] |
Cells are seeded into 96- or 384-well plates at densities ranging from 10,000 to 30,000/cm2 for adherent and 100,000/mL for nonadherent cells in appropriate medium supplemented with 10% fetal calf serum. After 24 hours, cells are treated in duplicate with serial dilutions of NMS-P937, and 72 hours later, the viable cell number is assessed by the CellTiter-Glo Assay. IC50 values are calculated with a sigmoidal fitting algorithm. Experiments are carried out independently at least twice. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
Animal Administration [2] |
For carcinoma xenograft studies, 5- to 6-week-old female Hsd, athymic nu/nu mice (average weight, 20-22 g), are used. HCT116, HT29, Colo205 colorectal, and A2780 ovarian human carcinoma cell lines are inoculated subcutaneously. Mice bearing a palpable tumor (100-200 mm3) are treated with vehicle or NMS-P937 following doses and schedules starting from the day after randomization. Tumor dimensions are measured regularly with Vernier calipers, and tumor growth inhibition (TGI) is calculated. Toxicity is evaluated on the basis of body weight reduction. For leukemia studies, 5- to 6-week-old female severe combined immunodeficient mice (SCID; average weight, 20-22 g) are used. The AmL cell line HL-60 (5×106 cells) is injected subcutaneously and treatments initiated when tumor size reaches 200 to 250 mm3. Tumor dimensions and TGI are assessed. For disseminated models, 5×106 AmL primary cells (AmL-PS) are injected intravenously and treatments start after 2 days. Mice are monitored daily for clinical signs of disease, and the median survival time is determined for each group. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
|
所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务