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RP-6306
- Lunersertib
- Optical Purity: 100% e.e.
- Soluble in 0.1N HCl(aq), DMSO and EtOH
- MF: C18H20N4O2
- MW: 324.38
Description
RP-6306 is a first-in-class, potent, selective, and orally bioavailable PKMYT1 (or MYT1) inhibitor with IC50 values of 0.014 μM and 0.002 μM in cell and nanoBRET assays, respectively. RP-6306 is the active (aS)-atropisomer of the racemate. Its opposite atropisomer, (aR)-RP-6306 (Axon 3759), is also available.
In a recent study, Wee1 inhibitor MK-1775 (Axon 1494) and MYT1 inhibitor RP-6306 (Axon 3668) combination treatment showed synergistic cell killing in a panel of cancer cell lines. Wee1 and MYT1 combined inhibition might be a potential cancer therapeutic strategy.
More Information
| Parent CAS No. | 2719793-90-3 |
|---|---|
| Chemical Name | (S)-2-Amino-1-(3-hydroxy-2,6-dimethyl-phenyl)-5,6-dimethylpyrrolo[2,3-b]pyridine-3-carboxamide |
| SMILES | C12C(C(=O)N)=C(N)N(C3=C(C)C(O)=CC=C3C)C1=NC(C)=C(C)C=2 |
| MFCD | N.A. |
| 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 |
| CID | 156869388 |
| Short Description | PKMYT1 inhibitor |
References
- D Gallo et al. CCNE1 amplification is synthetic lethal with PKMYT1 kinase inhibition. Nature. 2022 Apr;604(7907):749-756.
- J Szychowski et al. Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor, RP-6306. J Med Chem. 2022 Aug 11;65(15):10251-10284.
- S Sokhi et al. Investigating Wee1 and Myt1 combined inhibition as a potential cancer therapeutic strategy. [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2023; Part 1 (Regular and Invited Abstracts); 2023 Apr 14-19; Orlando, FL. Philadelphia (PA): AACR; Cancer Res 2023;83(7_Suppl):Abstract nr 5511.
Related Products
| AXON ID | NAME | FROM PRICE |
|---|---|---|
| 1494 | MK 1775 |
From $88.00 |
| 3759 | (aR)-RP-6306 |
From $198.00 |
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