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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $133 | In Stock | |
5 mg | $329 | In Stock | |
10 mg | $488 | In Stock | |
25 mg | $786 | In Stock | |
50 mg | $1,090 | In Stock | |
1 mL x 10 mM (in DMSO) | $587 | In Stock |
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. |
Targets&IC50 | PKMYT1:14 nM |
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] |
Alias | (S)-RP-6306 |
Molecular Weight | 324.38 |
Formula | C18H20N4O2 |
Cas No. | 2719793-90-3 |
Smiles | NC=1N(C=2C(C1C(N)=O)=CC(C)=C(C)N2)C3=C(C)C(O)=CC=C3C |
Storage | keep away from direct sunlight,keep away from moisture,store at low temperature | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 45.0 mg/mL (138.7 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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