RP 6306

RP 6306 is an inhibitor of membrane-associated tyrosine- and threonine-specific Cdc2-inhibitory kinase (Myt1 kinase), also known as PKMYT1 (IC50 = 0.002 nM in a bioluminescence resonance energy transfer (BRET) assay). It is greater than 29-fold selective for Myt1 kinase over eight other kinases in BRET assays at 1.2 µM. RP 6306 (500 nM) increases the levels of DNA-associated gamma histone H2AX (gammaH2AX), a marker of DNA damage, in hTERT FT 282 fallopian tube cells. It induces cell cycle arrest at the S phase in hTERT FT 282 cells. Dietary administration of RP 6306 (15, 50, or 300 ppm) reduces tumor volume in an OVCAR-3 ovarian cancer mouse xenograft model.Formal Name: (1S)-2-amino-1-(3-hydroxy-2,6-dimethylphenyl)-5,6-dimethyl-1H-pyrrolo[2,3-b]pyridine-3-carboxamide. CAS Number: 2719793-90-3. Synonyms: Lunresertib, (S)-RP 6306. Molecular Formula: C18H20N4O2. Formula Weight: 324.4. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Sparingly soluble: 1-10 mg/ml. SMILES: O=C(C1=C(N)[N@]([C@]2=C(C)C(O)=CC=C2C)C3=NC(C)=C(C)C=C31)N. InChi Code: 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). InChi Key: ARBRHWRTXPWZGN-UHFFFAOYSA-N.