D16-M1P2 |
D16-M1P2 : Degrader (PROTAC) of PKMYT1
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| PKMYT1 |
|
|
Degrader (PROTAC)
30-50 nM
10 nM, up to 100 nM hock effect observed around 1000 nM
Selectivity
In Vitro Selectivity Assessment
Potency Assay Off-Target:
KinomeScan of 403 non-mutant kinases performed at 1 uM.
Selectivity Assessment Description:
Only 4 of the 403 kinases tested, including PKMYT1, exceeded 65% inhibition at 1000 nM (130× its enz ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
D16-M1P2 was profiled in HCC1569 cells following 8-hour treatment with 10 and 100 nM. Analysis quant ...
Potency Cellular
In Vitro
PKMYT1
Mode of Action: Degrader (PROTAC)
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1038/s41467-025-65796-8
In Vivo Validations
Mouse
Dose: 1 mg/Kg IV, 40 mg/Kg PO
Route of delivery:
Intravenous, Oral
Plasma half life:
3.6 h
Systemic clearance:
80.2 mL/min/Kg
Cmax:
1181 ng/mL
Area Under the Curve::
7436 h*ng/mL
Bioavailability:
91.3%
Volume of Distribution at Steady-State:
6.6 L/Kg
DOI Reference: 10.1038/s41467-025-65796-8
Rat
Dose: 1 mg/Kg IV, 20 mg/Kg PO
Route of delivery:
Intravenous, Oral
Plasma half life:
7.7 h
Systemic clearance:
17.6 mL/min/Kg
Cmax:
2269 ng/mL
Area Under the Curve::
29851 h*ng/mL
Bioavailability:
166.5%
Volume of Distribution at Steady-State:
3.7 L/Kg
DOI Reference: 10.1038/s41467-025-65796-8
Dog
Dose: 1 mg/Kg IV, 5 mg/Kg PO
Route of delivery:
Intravenous, Oral
Plasma half life:
6.3 h
Systemic clearance:
7.2 mL/min/Kg
Cmax:
583 ng/mL
Area Under the Curve::
7461 h*ng/mL
Bioavailability:
67.9%
Volume of Distribution at Steady-State:
3.3 L/Kg
DOI Reference: 10.1038/s41467-025-65796-8
Monkey (Cynomolgus)
Dose: 1 mg/Kg IV, 10 mg/Kg PO
Route of delivery:
Intravenous, Oral
Plasma half life:
10.9 h
Systemic clearance:
19.3 mL/min/Kg
Cmax:
144 ng/mL
Area Under the Curve::
1721 h*ng/mL
Bioavailability:
20.5%
Volume of Distribution at Steady-State:
5.1 L/Kg
DOI Reference: 10.1038/s41467-025-65796-8
Negative Control Compounds
D16-NMe-M1P2
Notes: D16-NMe-M1P2 retained similar PKMYT1 enzymatic inhibition (IC50 of 8.5 nM) and intracellular target engagement (EC50 of 8.0 nM) to D16-M1P2 with DC50 >1000 nM.
SMILES:
CC1=C(C(=C(C=C1)O)C)C2=C(C#N)C3=C(N=C2)NC(=C3)C4=CN=C(N=C4)N5CCC6(CC5)CC(CO6)N7CCN(CC7)C8=CC=C(C=C8F)N[C@H]9CCC(=O)N(C)C9=O
Chemical Information
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