RP 6306

Key Product Details

Product Description

RP 6306 (Lunresertib) is a potent and selective PKMYT1 inhibitor (IC₅₀ = 2 nM in a BRET assay and IC₅₀ = 14 nM in a cellular assay). It displays selectivity for PKMYT1 over ephrin type-B EPHB3 (selectivity ratio = 131). It also shows greater than 29-fold selectivity for PKMYT1 over eight other kinases in BRET assays at 1.2 µM.

RP 6306 promotes early mitosis in cells undergoing DNA synthesis by causing unscheduled activation of CDK1 selectively in CCNE1-overexpressing cells. RP 6306 targets CCNE1-amplified tumor cells and shows enhanced efficacy when combined with Gemcitabine (Cat. No. 3259) or hydroxyurea.

In vivo, it inhibits CCNE1-amplified tumor cell growth in mouse xenograft models. RP 6306 is orally bioavailable.

Product Specifications for RP 6306

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for RP 6306

The following data is based on the product molecular weight 324.38.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	3.08 mL	15.41 mL	30.83 mL
5 mM	0.62 mL	3.08 mL	6.17 mL
10 mM	0.31 mL	1.54 mL	3.08 mL
50 mM	0.06 mL	0.31 mL	0.62 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Szychowski Discovery of an orally bioavailable and selective PKMYT1 inhibitor, RP-6306. J.Med.Chem. 2022 PMID: 35880755
• Gallo CCNE1 amplification is synthetic lethal with PKMYT1 kinase inhibition. Nature 2022 PMID: 35444283

Product Documents for RP 6306