An Myt1 kinase inhibitor
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Isomer(s)
41738(R)-RP 6306
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RP 6306

Item No. 41732

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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(Learn about Variance in 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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $98

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    10 mg

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    25 mg

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    50 mg

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    Product Description

    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).1 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 γ histone H2AX (γH2AX), a marker of DNA damage, in hTERT FT 282 fallopian tube cells.2 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.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Szychowski, J., Papp, R., Dietrich, E., et al. Discovery of an orally bioavailable and selective PKMYT1 inhibitor, RP-6306. J. Med. Chem. 65(15), 10251-10284 (2022).

    2. Gallo, D., Young, J.T.F., Fourtounis, J., et al. CCNE1 amplification is synthetic lethal with PKMYT1 kinase inhibition. Nature 604(7907), 749-756 (2022).