RP-6306
- Product Name
- RP-6306
- CAS No.
- 2719793-90-3
- Chemical Name
- RP-6306
- Synonyms
- RP-6306;lunresertib;Iunresertib;RP-6306 ，E1175;RP-6306, 10 mM in DMSO;2-Amino-1-(3-hydroxy-2,6-dimethylphenyl)-5,6-dimethyl-7-azaindole-3-carboxamide;2-amino-1-(3-hydroxy-2,6-dimethyl-phenyl)-5,6-dimethyl-pyrrolo[2,3-b]pyridine-3-carboxamide;(1S)-2-Amino-1-(3-hydroxy-2,6-dimethylphenyl)-5,6-dimethyl-1H-pyrrolo[2,3-b]pyridine-3-carboxamide;1H-Pyrrolo[2,3-b]pyridine-3-carboxamide, 2-amino-1-(3-hydroxy-2,6-dimethylphenyl)-5,6-dimethyl-, (1S)-
- CBNumber
- CB310855776
- Molecular Formula
- C18H20N4O2
- Formula Weight
- 324.38
- MOL File
- 2719793-90-3.mol
RP-6306 Property
- Boiling point:
- 489.2±45.0 °C(Predicted)
- Density
- 1.36±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: Sparingly soluble: 1-10 mg/ml
- pka
- 9.20±0.23(Predicted)
- form
- Solid
- color
- Off-white to gray
- InChI
- InChI=1S/C18H20N4O2/c1-8-5-6-13(23)10(3)15(8)22-16(19)14(17(20)24)12-7-9(2)11(4)21-18(12)22/h5-7,23H,19H2,1-4H3,(H2,20,24)
- InChIKey
- ARBRHWRTXPWZGN-UHFFFAOYSA-N
- SMILES
- NC1=C(C2=CC(C)=C(C)N=C2N1C1C(=CC=C(O)C=1C)C)C(=O)N
RP-6306 Chemical Properties,Usage,Production
Uses
lunresertib (RP-6306) is a potent, selective and orally active PKMYT1 inhibitor with an IC50 of 14 nM. lunresertib shows a high degree of selectivity over other kinases in cellular binding assays. lunresertib shows anticancer effects[1].
in vivo
lunresertib (15, 50, and 300 ppm; oral; daily; for 21 days) results in a statistically significant and dose-dependent reduction in OVCAR3 tumor growth in CCNE1-amplified ovarian xenograft model (OVCAR3)[1].
| Animal Model: | OVCAR3-bearing mice[1] |
| Dosage: | 15, 50, and 300 ppm (equivalent to approximately 3, 10, and 60 mg/kg/day) |
| Administration: | Oral; daily; for 21 days |
| Result: | Resulted in a statistically significant and dose-dependent reduction in OVCAR3 tumor growth. |
IC 50
PKMYT1: 14 nM (IC50)
References
[1] Janek Szychowski, et al. Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor, RP-6306. J Med Chem. 2022 Aug 11;65(15):10251-10284. DOI:10.1021/acs.jmedchem.2c00552
[2] David Gallo, et al. CCNE1 amplification is synthetic lethal with PKMYT1 kinase inhibition. Nature. 2022 Apr;604(7907):749-756. DOI:10.1038/s41586-022-04638-9
RP-6306 Preparation Products And Raw materials
Raw materials
Preparation Products
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