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RP-6306 | RP-6306 : Inhibitor of PKMYT1
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
PKMYT1
  • IC50:< 10 nM
  • IC50:14 nM
  • IC50:2 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
RP-6306 was tested in a Kinativ Colo-205 cell lysate kinase binding assay at 1.2 μM binding to only ...

Potency
Cellular
In Vitro

PKMYT1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.2c00552

In Vivo Validations

Rat
Dose: 1 mg/Kg IV, 2.5 or 5 mg/Kg PO
Route of delivery: Intravenous, Oral
Systemic clearance: 198 mL/min/kg
Fb : 87.7%
Bioavailability: 48%
Target engagement assay: Potent in vivo PKMYT1 target inhibition and direct relationship between RP-6306 free plasma levels and tumor pCDK1(Thr14) inhibition: EC50 to inhibit pCDK1(Thr14) by 50% was calculated as 0.20 nM and EC90 as 11 nM.

DOI Reference: 10.1021/acs.jmedchem.2c00552

Negative Control Compounds

Cpd 4
Notes: In cell IC50 > 3 uM
SMILES: NC(C1=C(N)N(C2=CC=CC(O)=C2C)C3=NC4=C(C=CC=C4)N=C31)=O

Chemical Information

Molecular Formula C18H20N4O2
SMILEs Cc1cc2c(C(N)=O)c(N)n(-c3c(C)ccc(O)c3C)c2nc1C
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)
Molecular weight 324.16 Da
AlogP 0.0
HBond acceptors 6
HBond donors 5
Atoms 44
PAINS * Yes

* This is an automated alert only, and may not necessarily indicate an issue with this probe. ( Learn more about PAINS )

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Expert Reviews

No SERP comments found for RP-6306

Probe RP-6306 is in the process of SERP review.

Please continue to check back for new reviews and commentary.