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Nedisertib

Catalog No. TQ0031 CAS 1637542-33-6

Synonyms: M3814

Nedisertib (M3814) is a specific inhibitor of DNA-dependent Protein Kinase (DNA-PK, IC50: <3 nM).

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Nedisertib, CAS 1637542-33-6

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Nedisertib (M3814) is a specific inhibitor of DNA-dependent Protein Kinase (DNA-PK, IC50: <3 nM).
Targets&IC50	DNA-PK:<3 nM
In vitro	Nedisertib is a DNA-PK inhibitor, with an IC50 of <3 nM for DNA-PK and <0.5 μΜ for cellular pDNA-PK [2].
In vivo	In combination with IR, Nedisertib shows efficacy in all of the 6 mouse models of human cancer. Nedisertib, alone or in combination with IR, does not induce significant weight loss or visual signs of toxicity in the mice in any study. In all models, a dose of 2 Gy administered daily for 1 week in combination with Nedisertib induces statically significant tumor growth inhibition to compare to IR alone [1].
Animal Research	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 [1].

Synonyms	M3814
Molecular Weight	481.91
Formula	C24H21ClFN5O3
CAS No.	1637542-33-6

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 100 mg/mL (207.51 mM), Need ultrasonic

H2O: Insoluble

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. L. Damstrup, et al. M3814, a DNA-dependent Protein Kinase Inhibitor (DNA-PKi), Potentiates the Effect of Ionizing Radiation (IR) in Xenotransplanted Tumors in Nude Mice. IJROBP. 2016; 94, 940-941. 2. Thomas Fuchss, et al. Arylchinazoline. WO2014183850A1.

Citations

1. Ma X, Yao M, Gao Y, et al. Functional Immune Cell‐Derived Exosomes Engineered for the Trilogy of Radiotherapy Sensitization. Advanced Science. 2022: 2106031

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library Preclinical Compound Library Anti-Lung Cancer Compound Library Inhibitor Library DNA Damage & Repair Compound Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Kinase Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library

Related Products

Related compounds with same targets

DMNB AZD-7648 OSI-027 SF2523 CC-115 ETP-45658 PIK-75 hydrochloride PI-3065

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Nedisertib 1637542-33-6 DNA Damage/DNA Repair PI3K/Akt/mTOR signaling DNA-PK M3814 Inhibitor inhibitor inhibit

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