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Chemical Structure : RP-3500
CAS No.: 2417489-10-0
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 1 mg | $178 | In stock | |
| 5 mg | $398 | In stock | |
| 10 mg | $598 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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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.
| M.Wt | 410.478 | |
| Formula | C21H26N6O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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1. Anne Roulston, et al. Mol Cancer Ther. 2022 Feb;21(2):245-256.
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