| Chemical Properties | Back Directory | [Boiling point ]
489.2±45.0 °C(Predicted) | [density ]
1.36±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: Sparingly soluble: 1-10 mg/ml | [form ]
Solid | [pka]
9.20±0.23(Predicted) | [color ]
Off-white to gray | [InChI]
InChI=1S/C18H20N4O2/c1-8-5-6-13(23)10(3)15(8)22-16(19)14(17(20)24)12-7-9(2)11(4)21-18(12)22/h5-7,23H,19H2,1-4H3,(H2,20,24) | [InChIKey]
ARBRHWRTXPWZGN-UHFFFAOYSA-N | [SMILES]
NC1=C(C2=CC(C)=C(C)N=C2N1C1C(=CC=C(O)C=1C)C)C(=O)N |
| Hazard Information | Back Directory | [Uses]
lunresertib (RP-6306) is a potent, selective and orally active PKMYT1 inhibitor with an IC50 of 14 nM. lunresertib shows a high degree of selectivity over other kinases in cellular binding assays. lunresertib shows anticancer effects[1]. | [in vivo]
lunresertib (15, 50, and 300 ppm; oral; daily; for 21 days) results in a statistically significant and dose-dependent reduction in OVCAR3 tumor growth in CCNE1-amplified ovarian xenograft model (OVCAR3)[1]. | Animal Model: | OVCAR3-bearing mice[1] | | Dosage: | 15, 50, and 300 ppm (equivalent to approximately 3, 10, and 60 mg/kg/day) | | Administration: |
Oral; daily; for 21 days | | Result: | Resulted in a statistically significant and dose-dependent reduction in OVCAR3 tumor growth.
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| [IC 50]
PKMYT1: 14 nM (IC50) | [storage]
Store at -20°C | [References]
[1] Janek Szychowski, et al. Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor, RP-6306. J Med Chem. 2022 Aug 11;65(15):10251-10284. DOI:10.1021/acs.jmedchem.2c00552
[2] David Gallo, et al. CCNE1 amplification is synthetic lethal with PKMYT1 kinase inhibition. Nature. 2022 Apr;604(7907):749-756. DOI:10.1038/s41586-022-04638-9 |
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