Nedisertib (M3814)

製品コードS8586 バッチS858602

印刷

化学情報

Synonyms

Peposertib, MSC2490484A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₄H₂₁ClFN₅O₃

分子量

481.91

CAS No.

1637542-33-6

Solubility (25°C)*

体外

DMSO

48 mg/mL (99.6 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Nedisertib (M3814, Peposertib, MSC2490484A) is an orally bioavailable, highly potent and selective inhibitor of DNA activated protein kinase (DNA-PK) with IC50 of < 3 nM.
in vitro	Nedisertib (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 by this compound leads to an increased number of persistent DSBs.^[2]
in vivo	Inhibition of DNA-PK autophosphorylation in xenograft tumors leads to an increased number of persistent DSBs. Oral administration of this compound 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.^[2]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	92 cancer cell lines and resting peripheral blood mononuclear cells (PBMCs)
	濃度	5 μmol/L–5 nmol/L
	反応時間	120 h
	実験の流れ	Radiosensitization of 92 cancer cell lines and resting peripheral blood mononuclear cells (PBMCs) by Nedisertib (M3814) is performed at Oncolead. Cell viability is determined with 3 Gy IR, this compound (5 μmol/L–5 nmol/L), and a combination of 3 Gy IR and it (5 μmol/L–5 nmol/L). Treated cells are incubated for 120 hours, fixed, stained with sulforhodamine B, and quantified colorimetrically.
動物実験	動物モデル	7- to 9-week-old female NMRI (nu/nu) mice
	投薬量	5 mg/kg, 25 mg/kg, 100 mg/kg
	投与方法	Oral gavage

参考

https://patents.google.com/patent/WO2014183850A1/en
https://pubmed.ncbi.nlm.nih.gov/32220971/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

A redefined InDel taxonomy provides insights into mutational signatures [ Nat Genet, 2025, 57(5):1132-1141]	PubMed: 40210680
Tumor site-directed A1R expression enhances CAR T cell function and improves efficacy against solid tumors [ Nat Commun, 2025, 16(1):6123]	PubMed: 40610421
Targeting synthetic lethality between non-homologous end joining and radiation in very-high-risk medulloblastoma [ Cell Rep Med, 2025, 6(7):102202]	PubMed: 40562042
Post-cleavage target residence determines asymmetry in non-homologous end joining of Cas12a-induced DNA double strand breaks [ Genome Biol, 2025, 26(1):96]	PubMed: 40229905
Rescue of the disease-associated phenotype in CRISPR-corrected hiPSCs as a therapeutic approach for inherited retinal dystrophies [ Mol Ther Nucleic Acids, 2025, 36(1):102482]	PubMed: 40083649
Loss of genome maintenance is linked to mTOR complex 1 signaling and accelerates podocyte damage [ JCI Insight, 2025, 10(12)e172370]	PubMed: 40392611
Extracellular Mitochondria Exacerbate Retinal Pigment Epithelium Degeneration in Diabetic Retinopathy [ Diabetes, 2025, 74(3):409-415]	PubMed: 39715576
DDX1 is required for non-spliceosomal splicing of tRNAs but not of XBP1 mRNA [ Commun Biol, 2025, 8(1):92]	PubMed: 39833356
DNA-PK inhibition sustains the antitumor innate immune response in small cell lung cancer [ iScience, 2025, 28(3):111943]	PubMed: 40034862
Efficient nonviral integration of large transgenes into human T cells using Cas9-CLIPT [ Mol Ther Methods Clin Dev, 2025, 33(1):101437]	PubMed: 40123742

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。