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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-ATM/ATR-AD1058
AD1058

Chemical Structure : AD1058

CAS No.: 2907782-78-7

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AD1058 (AD-1058)

货号: PC-22828Not For Human Use, Lab Use Only.

AD1058 is a highly potent, selective, brain-penetrant ATR inhibitor with IC50 of 1.6 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

AD1058 is a highly potent, selective, brain-penetrant ATR inhibitor with IC50 of 1.6 nM.
AD1058 displays excellent selectivity against 15 kinases belonging to six kinase subfamilies (mTOR from PIKK subfamily; AMPKα2β1γ1, DRAK2, BRSK2, ARK5 from CAMK subfamily; CDK2 from CMGC subfamily; IRAK4 from TKL subfamily; FLT3, LCK, MER, LYN, BTK, ABL1, JAK1 from TK subfamily; Aurora B from Aurora subfamily).
AD1058 exhibits potent in vitro antiproliferative activities against a panel of tumor cell lines (B-cell lymphoma: Granta-519 (IC50=0.19 uM), OCI-Ly10, SU-DHL4, ovary cancer: A2780, colorectal cancer: LoVo, HCT116, HT-29, DLD1, lung cancer: NCI-H446, pancreatic cancer: Capan-1, and prostate cancer: PC-3).
AD1058 effectively inhibits Niraparib-induced CHK1 phosphorylation in Granta-519, more potently than AZ20 or AZD6738 at 2 uM. AD1058 (25 and/or 50 mg/kg) exhibits significant inhibition of tumor growth in CB17-SCID mice bearing xenograft tumor inoculating Granta-519, effectively improves the antitumor effect of the clinically ionizing radiotherapy.

物理化学性质&存储条件

分子量 412.47
分子式 C19H20N6O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(R)-3-Methyl-4-(7-(methylsulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)morpholine

参考文献

1. Liu Z, et al. J Med Chem. 2024 Jul 25. doi: 10.1021/acs.jmedchem.4c00734.

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