| Name | RP-6306 |
| Description | Lunresertib (RP-6306) is a potent, selective, and orally active PKMYT1 inhibitor with an IC50 of 14 nM. Lunresertib (RP-6306) inhibits the growth of CCNE1-amplified tumor cells in several preclinical xenograft models. |
| In vitro | METHODS: HCC1569 breast cancer cell line was treated with lunresertib (RP-6306) (63, 125, 250, 500 nM) to assess whether PKMYT1 inhibition leads to DNA damage in CCNE1-high cells by monitoring γH2AX levels using quantitative image-based flow cytometry.
RESULTS Treatment with lunresertib (RP-6306) induced pan-γH2AX in the HCC1569 breast cancer cell line, suggesting that tumor-derived CCNE1 amplification also renders cells susceptible to DNA damage induction following PKMYT1 inhibition. [1] |
| In vivo | METHODS: lunresertib (RP-6306) (3, 10 and 60 mg/kg, oral, daily) was used to treat CCNE1-amplified ovary xenograft model (OVCAR3) mice, and tumor growth in the mice was observed.
RESULTS lunresertib (RP-6306) inhibited tumor growth in OVCAR3 mice in a statistically significant concentration-dependent manner. [2] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 67.3 mg/mL (207.47 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (6.17 mM), Sonication is recommended.
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| Keywords | RP-6306 | RP6306 | RP 6306 | PKMYT1 |
| Inhibitors Related | ZN-c3 | (R)-Lunresertib | GSK-1520489A | PF-06651481-00 | PD0166285 | ZNL 02-096 | Adavosertib | Debio-0123 | WEE1-IN-10 | Griseofulvin | WEE1-IN-3 | PD173952 |
| Related Compound Libraries | ReFRAME Related Library | Kinase Inhibitor Library | Anti-Breast Cancer Compound Library | Post-Translational Modification Compound Library | Inhibitor Library | Orally Active Compound Library | Cell Cycle Compound Library |
United States
