RP 6306
Tocris Bioscience, part of Bio-Techne | Catalog # 8031
Potent and selective PKMYT1 inhibitor
Key Product Details
Description
Potent and selective PKMYT1 inhibitor
Alternative Names
Lunresertib
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
Molecular Weight
324.38
Formula
C18H20N4O2
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
(S)-2-Amino-1-(3-hydroxy-2,6-dimethylphenyl)-5,6-dimethylpyrrolo[2,3-b]pyridine-3-carboxamide
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
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 Specific Notices for RP 6306
For research use only
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