For research use only. Not for therapeutic Use.
RP-6306 ((S)-RP-6306) is a potent, selective and orally active PKMYT1 inhibitor with an IC50 of 14 nM. RP-6306 shows a high degree of selectivity over other kinases in cellular binding assays. RP-6306 shows anticancer effects[1].
RP-6306 (500 nM; for 24 h) treatment induces pan-γH2AX in an HCC1569 breast cancer cell line, indicating that tumour-derived CCNE1 amplification also renders cells vulnerable to DNA damage induction following PKMYT1 inhibition[2].
RP-6306 treatment causes unscheduled activation of CDK1 selectively in CCNE1-overexpressing cells, promoting early mitosis in cells undergoing DNA synthesis[2].
RP-6306 (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].
| Catalog Number | I043977 |
| CAS Number | 2719793-90-3 |
| Synonyms | 2-amino-1-(3-hydroxy-2,6-dimethylphenyl)-5,6-dimethylpyrrolo[2,3-b]pyridine-3-carboxamide |
| Molecular Formula | C18H20N4O2 |
| Purity | ≥95% |
| 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 | CC1=C(C(=C(C=C1)O)C)N2C(=C(C3=C2N=C(C(=C3)C)C)C(=O)N)N |
| Reference | [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. [2]. David Gallo, et al. CCNE1 amplification is synthetic lethal with PKMYT1 kinase inhibition. Nature. 2022 Apr;604(7907):749-756. |
