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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-ATM/ATR-RP-3500
RP-3500

Chemical Structure : RP-3500

CAS No.: 2417489-10-0

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RP-3500 (RP3500, Camonsertib)

货号: PC-72315Not For Human Use, Lab Use Only.

RP-3500 (RP3500, Camonsertib) is a novel potent, selective, orally bioavailable ATR inhibitor with IC50 of 1.0 and 0.33 nM in biochemical and cell-based assays, respectively.

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1 mg ￥1780 In stock
5 mg ￥3980 In stock
10 mg ￥5980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

RP-3500 (RP3500, Camonsertib) is a novel potent, selective, orally bioavailable ATR inhibitor with IC50 of 1.0 and 0.33 nM in biochemical and cell-based assays, respectively.
RP-3500 displays 30-fold selectivity over mTOR and >2,000-fold selectivity over ATM, DNA-PK, and PI3Kα kinases.
RP-3500 inhibited phosphorylated checkpoint kinase 1 (pCHK1) (IC80=18.6 nM) and induction of phosphorylated H2A.X variant histone (γH2AX), phosphorylated DNA-PK catalytic subunit (pDNA-PKcs), and phosphorylated KRAB-associated protein 1 (pKAP1).
RP-3500 demonstrated potent single-agent efficacy and/or tumor regression in multiple xenograft models at minimum effective doses (MED) of 5 to 7 mg/kg once daily.
RP-3500 demonstrated superior efficacy when combined with PARP inhibitor olaparib or niraparib.

物理化学性质&存储条件

分子量 410.478
分子式 C21H26N6O3
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

(1R,3r,5S)-3-(6-((R)-3-methylmorpholino)-1-(1H-pyrazol-3-yl)-1H-pyrazolo[3,4-b]pyridin-4-yl)-8-oxabicyclo[3.2.1]octan-3-ol

参考文献

1. Anne Roulston, et al. Mol Cancer Ther. 2022 Feb;21(2):245-256.

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