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Chemical Structure : RP-6306
CAS No.: 2719793-90-3
Catalog No.: PC-73399Not For Human Use, Lab Use Only.
RP-6306 (Lunresertib, RP6306) is a first-in-class, potent and selective, orally available inhibitor of PKMYT1 with IC50 of 2.4 nM, displays less potency (>35-fold) against EphA1-2, and EphB2-4, and Wee1.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 2 mg | $248 | In stock | |
| 5 mg | $398 | In stock | |
| 10 mg | $598 | In stock | |
| 25 mg | Get quote | ||
| 100 mg | Get quote |
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RP-6306 (Lunresertib, RP6306) is a first-in-class, potent and selective, orally available inhibitor of PKMYT1 with IC50 of 2.4 nM, displays less potency (>35-fold) against EphA1-2, and EphB2-4, and Wee1.
RP-6306 inhibits the phosphorylation of CDK1 Thr14 in vivo in tumor tissue and inhibits CCNE1-amplified tumor cell growth in several preclinical xenograft models.
PKMYT1 is an important regulator of CDK1 phosphorylation and is a compelling therapeutic target for the treatment of certain types of DNA damage response cancers due to its established synthetic lethal relationship with CCNE1 amplification.
PKMYT1 is a member of the Wee-kinase family protein kinases, PKMYT1 is involved in G2/M checkpoint regulation of the cell cycle.
| M.Wt | 324.384 | |
| Formula | C18H20N4O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(1S)-2-Amino-1-(3-hydroxy-2,6-dimethylphenyl)-5,6-dimethyl-1H-pyrrolo[2,3-b]pyridine-3-carboxamide |
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1. Janek Szychowski, et al. Discovery of an orally bioavailable and selective PKMYT1 inhibitor RP-6306. ChemRxiv. DOI 10.26434/chemrxiv-2022-2g6m6.
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