Nedisertib

99.00%

Nedisertib

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品牌：源叶(MedMol)

产品编号：S89255 一键复制产品信息

CAS号：1637542-33-6

分子式：C₂₄H₂₁ClFN₅O₃

分子量：481.9066432

别名：(S)-(2-chloro-4-fluoro-5-(7-morpholinoquinazolin-4-yl)phenyl)(6-methoxypyridazin-3-yl)methanol；MSC2490484A; MSC-2490484A; MSC 2490484A; M3814; M-3814; M 3814; nedisertib; peposertib

货号	规格	价格	上海	北京	珠海	重庆	武汉
S89255-5mg	99.00%	￥480.00 S89255-5mg ￥480.00 现货	4 2 4	2	-	-	-
S89255-10mg	99.00%	￥700.00 S89255-10mg ￥700.00 现货	1 1	-	-	-	-
S89255-25mg	99.00%	￥1400.00 S89255-25mg ￥1400.00 现货	3 3	-	-	-	-
S89255-100mg	99.00%	￥4000.00 S89255-100mg ￥4000.00 现货	1 1	-	-	-	-

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产品介绍参考文献质检证书(COA) 摩尔浓度计算器相关产品

产品描述：

Nedisertib (M3814, Peposertib, MSC2490484A) 是一种口服可利用的、高效且选择性的 DNA activated protein kinase (DNA-PK) 的抑制剂，其IC50值小于3 nM

靶点：

DNA-PK(Cell-free assay):3 nM

体外研究：

M3814 potently inhibits DNA-PK catalytic activity and sensitizes multiple cancer cell lines to ionizing radiation (IR) and DSB-inducing agents. Inhibition of DNA-PK autophosphorylation in cancer cells leads to an increased number of persistent DSBs

体内研究：

Inhibition of DNA-PK autophosphorylation in xenograft tumors leads to an increased number of persistent DSBs. Oral administration of M3814 to two xenograft models of human cancer, using a clinically established 6-week fractionated radiation schedule, strongly potentiates the antitumor activity of IR and lead to complete tumor regression at nontoxic doses

细胞实验：

Cell lines: 92 cancer cell lines and resting peripheral blood mononuclear cells (PBMCs) Concentrations: 5 μmol/L–5 nmol/L Incubation Time: 120 h Method: Radiosensitization of 92 cancer cell lines and resting peripheral blood mononuclear cells (PBMCs) by M3814 is performed at Oncolead. Cell viability is determined with 3 Gy IR, M3814 (5 μmol/L–5 nmol/L), and a combination of 3 Gy IR and M3814 (5 μmol/L–5 nmol/L). Treated cells are incubated for 120 hours, fixed, stained with sulforhodamine B, and quantified colorimetrically.

动物实验：

Animal Models: 7- to 9-week-old female NMRI (nu/nu) mice Dosages: 5 mg/kg, 25 mg/kg, 100 mg/kg Administration: Oral gavage

参考文献：

1. Thomas Fuchss, et al. WO2014183850A1. 2. Frank T Zenke, et al. Pharmacologic Inhibitor of DNA-PK, M3814, Potentiates Radiotherapy and Regresses Human Tumors in Mouse Models. Mol Cancer Ther. 2020 May;19(5):1091-1101.

溶解性：

Soluble in DMSO、Ethanol

保存条件：

2-8℃

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
50 mM	0.042 ml	0.208 ml	0.415 ml