RP 6306

Name: RP 6306
Brand: Tocris Bioscience
SKU: 8031

Tocris Bioscience, part of Bio-Techne | Catalog # 8031

Citations (2)

COA / SDS

Potent and selective PKMYT1 inhibitor

Key Product Details

Description:	Potent and selective PKMYT1 inhibitor
Alternative Names:	Lunresertib
Chemical Name:	(S)-2-Amino-1-(3-hydroxy-2,6-dimethylphenyl)-5,6-dimethylpyrrolo[2,3-b]pyridine-3-carboxamide
Purity:	≥98% (HPLC)
Molecular Weight:	324.38

View Full Technical Details for RP 6306

Technical Data
Citations

Biological Activity for RP 6306

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.

Technical Data for RP 6306

M. Wt	324.38
Formula	C₁₈H₂₀N₄O₂
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	2719793-90-3
PubChem ID	156869388
InChi Key	ARBRHWRTXPWZGN-UHFFFAOYSA-N
Smiles	O=C(C1=C(N)N(C2=C(C)C(O)=CC=C2C)C3=C1C=C(C)C(C)=N3)N

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

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for RP 6306

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	32.44	100

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 will affect the solvent volumes required to prepare stock solutions.

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

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References for RP 6306

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