(αS)-α-[2-氯-4-氟-5-[7-(4-吗啉基)-4-喹唑啉基]苯基]-6-甲氧基-3-哒嗪甲醇

中文名	Nedisertib
英文名	Nedisertib
别名	化合物NEDISERTIB (αS)-α-[2-氯-4-氟-5-[7-(4-吗啉基)-4-喹唑啉基]苯基]-6-甲氧基-3-哒嗪甲醇
英文别名	M-3814 M3814 M 3814 M-3814 NEDISERTIB Nedisertib NEDISERTIB MSC2490484A MSC 2490484A MSC-2490484A M-3814(nedisertib) M3814 (MSC2490484A) (S)-(2-chloro-4-fluoro-5-(7-morpholinoquinazolin-4-yl)phenyl)(6-methoxypyridazin-3-yl)methanol 3-Pyridazinemethanol, α-[2-chloro-4-fluoro-5-[7-(4-morpholinyl)-4-quinazolinyl]phenyl]-6-methoxy-, (αS)-
CAS	1637542-33-6
化学式	C24H21ClFN5O3
分子量	481.91
密度	1.405±0.06 g/cm3(Predicted)
熔点	>198°C (dec.)
沸点	716.0±60.0 °C(Predicted)
溶解度	DMSO (轻微加热)，甲醇 (轻微超声处理)
酸度系数	11.35±0.20(Predicted)
存储条件	-20°C Freezer
外观	固体
颜色	Pale Yellow to Light Green
靶点	DNA-PK
参考资料展开查看	1: Fu YW, Dai XY, Wang WT, Yang ZX, Zhao JJ, Zhang JP, Wen W, Zhang F, Oberg KC, Zhang L, Cheng T, Zhang XB. Dynamics and competition of CRISPR-Cas9 ribonucleoproteins and AAV donor-mediated NHEJ, MMEJ and HDR editing. Nucleic Acids Res. 2021 Jan 25;49(2):969-985. doi: 10.1093/nar/gkaa1251. PMID: 33398341; PMCID: PMC7826255. 2: van Bussel MTJ, Awada A, de Jonge MJA, Mau-Sørensen M, Nielsen D, Schöffski P, Verheul HMW, Sarholz B, Berghoff K, El Bawab S, Kuipers M, Damstrup L, Diaz- Padilla I, Schellens JHM. A first-in-man phase 1 study of the DNA-dependent protein kinase inhibitor peposertib (formerly M3814) in patients with advanced solid tumours. Br J Cancer. 2021 Feb;124(4):728-735. doi: 10.1038/s41416-020-01151-6. Epub 2020 Nov 24. PMID: 33230210; PMCID: PMC7884679. 3: Wu ZX, Peng Z, Yang Y, Wang JQ, Teng QX, Lei ZN, Fu YG, Patel K, Liu L, Lin L, Zou C, Chen ZS. M3814, a DNA-PK Inhibitor, Modulates ABCG2-Mediated Multidrug Resistance in Lung Cancer Cells. Front Oncol. 2020 May 12;10:674. doi: 10.3389/fonc.2020.00674. PMID: 32477940; PMCID: PMC7235170. 4: Zenke FT, Zimmermann A, Sirrenberg C, Dahmen H, Kirkin V, Pehl U, Grombacher T, Wilm C, Fuchss T, Amendt C, Vassilev LT, Blaukat A. Pharmacologic Inhibitor of DNA-PK, M3814, Potentiates Radiotherapy and Regresses Human Tumors in Mouse Models. Mol Cancer Ther. 2020 May;19(5):1091-1101. doi: 10.1158/1535-7163.MCT-19-0734. Epub 2020 Mar 27. PMID: 32220971.

(αS)-α-[2-氯-4-氟-5-[7-(4-吗啉基)-4-喹唑啉基]苯基]-6-甲氧基-3-哒嗪甲醇 - 配置溶液浓度参考

	1mg	5mg	10mg
1 mM	2.075 ml	10.375 ml	20.751 ml
5 mM	0.415 ml	2.075 ml	4.15 ml
10 mM	0.208 ml	1.038 ml	2.075 ml
5 mM	0.042 ml	0.208 ml	0.415 ml

最后更新：2024-01-02 23:10:35

(αS)-α-[2-氯-4-氟-5-[7-(4-吗啉基)-4-喹唑啉基]苯基]-6-甲氧基-3-哒嗪甲醇 - 动物实验

The efficacy of Nedisertib in combination with IR is evaluated in 6 human xenograft models (NCI-H460, A549, HCT116, FaDu, Capan-1, BxPC3) in mice representing 4 different cancer types (colon, head and neck, lung, and pancreas). Tumor cells are injected s.c. into nude mice, and treatment starts when palpable tumors are established (~100 to 200 mm^3 ). Nedisertib is given orally at different doses (25 to 300 mg/kg) 10 min prior to IR. IR is applied using a radiation therapy device for small rodents calibrated to deliver 2 Gy. Autophosphorylation of DNA-PK (serine2056) in FaDu tumor lysates is measured by immunoassay to assess pharmacological inhibition by Nedisertib .

最后更新：2023-08-16 21:32:38

(αS)-α-[2-氯-4-氟-5-[7-(4-吗啉基)-4-喹唑啉基]苯基]-6-甲氧基-3-哒嗪甲醇 - 简介

Nedisertib是一种新型的小分子抑制剂，常用于肿瘤治疗。它的化学结构类似于丝裂霉素（paclitaxel）和去甲异慰春雷碱（vincristine）等天然产物。

Nedisertib可以通过抑制细胞内的Aurora激酶来抑制细胞的增殖和分裂。Aurora激酶是一类调控细胞有丝分裂进程的激酶，其异常活性常与肿瘤的发生和发展相关。

Nedisertib的合成方法一般使用有机合成化学方法，但其具体制法中的细节可能受到专有权限制。

Nedisertib的安全信息：目前尚未有非临床和临床研究结果公开报告。在进行临床试验之前，会对Nedisertib进行严格的毒理学评估以确定其毒性和安全性参数。

最后更新：2024-04-09 21:54:55

(αS)-α-[2-氯-4-氟-5-[7-(4-吗啉基)-4-喹唑啉基]苯基]-6-甲氧基-3-哒嗪甲醇

上海源叶生物科技有限公司

现货供应

产品名: Nedisertib 去供应商网站查看询盘
CAS: 1637542-33-6
产地: 上海
规格: 98%
价格: 5mg 1040,10mg 1600,25mg 3200,100mg 9600
库存: 现货
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产品描述: Nedisertib 98% MedMol 货号：S89255

上海源叶生物科技有限公司

现货供应

微信: 18301782025
产品描述: Nedisertib 98% MedMol 货号：S89255

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(αS)-α-[2-氯-4-氟-5-[7-(4-吗啉基)-4-喹唑啉基]苯基]-6-甲氧基-3-哒嗪甲醇

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