Camonsertib, also known as RP 3500, is aA Novel, Potent, and Selective ATR Inhibitor that is Effective in Preclinical Models as a Monotherapy and in Combination with PARP Inhibitors. RP-3500 is highly potent with IC50 values of 1.0 and 0.33 nmol/L in biochemical and cell-based assays, respectively. RP-3500 is highly selective for ATR with 30-fold selectivity over mammalian target of rapamycin (mTOR) and more than 2,000-fold selectivity over ataxia telangiectasia mutated (ATM), DNA-dependent protein kinase (DNA-PK), and phosphatidylinositol 3-kinase alpha (PI3Kα) kinases.
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| 名称 | Camonsertib |
|---|---|
| Iupac 化学名称 | (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 |
| 同义词 | Camonsertib; RP 3500; RP-3500; RP3500; |
| 英文同义词 | Camonsertib; RP 3500; RP-3500; RP3500; |
| 分子式 | C21H26N6O3 |
| 分子量 | 410.47 |
| Smile | O[C@@]1(C2=C3C(N(C4=NNC=C4)N=C3)=NC(N5[C@H](C)COCC5)=C2)C[C@@](O6)([H])CC[C@@]6([H])C1 |
| InChiKey | YIHHYCIYAIVQKX-MBIULKOWSA-N |
| InChi | InChI=1S/C21H26N6O3/c1-13-12-29-7-6-26(13)19-8-17(21(28)9-14-2-3-15(10-21)30-14)16-11-23-27(20(16)24-19)18-4-5-22-25-18/h4-5,8,11,13-15,28H,2-3,6-7,9-10,12H2,1H3,(H,22,25)/t13-,14-,15+,21+/m1/s1 |
| Cas号 | 2417489-10-0 |
| 相关CAS号 |
| 包装 | 价格 | 库存 | 纯度 | 备货期 |
|---|---|---|---|---|
| 大货 | 询价 | 询价 | 询价 |
| 外观性状 | 类白色固体 |
|---|---|
| 纯度 | 98% Min. |
| 存储 | 0-4℃,可保存几天到几周;-20℃,可保存 几个月。 |
| 可溶性 | 溶于DMSO等有机溶剂 |
| 处理方式 | Refer to MSDS |
| 运输条件 | 可以在室温下进行运输。 |
| 海关编码 | 2934200090 |
| Targets | |
|---|---|
| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
Roulston A, Zimmermann M, Papp R, Skeldon A, Pellerin C, Dumas-Bérube É, Dumais V, Dorich S, Fader LD, Fournier S, Li L, Leclaire ME, Yin SY, Chefson A, Alam H, Yang W, Fugère-Desjardins C, Vignini-Hammond S, Skorey K, Mulani A, Rimkunas V, Veloso A, Hamel M, Stocco R, Mamane Y, Li Z, Young JTF, Zinda M, Black WC. RP-3500: A Novel, Potent, and Selective ATR Inhibitor that is Effective in Preclinical Models as a Monotherapy and in Combination with PARP Inhibitors. Mol Cancer Ther. 2022 Feb;21(2):245-256. doi: 10.1158/1535-7163.MCT-21-0615. Epub 2021 Dec 15. PMID: 34911817.