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HM-279 | HM-279 : Inhibitor of TGFBR1
RATINGS:
Cellular Use: (0 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
TGFBR1
  • IC50:4.7 nM
  • IC50:21.6 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
ACVR1C

Gene ID: Q8NER5

Organism: Homo sapiens

Family: TKL Ser/Thr protein kinase family

Potency: IC50 - 6.8 nM

Potency Assay Off-Target:
HM-279 was evaluated in a panel of 10 TGF-β receptor family kinases. HM-279 showed cross-reactivity ...
In Vitro Selectivity Assessment
Potency Assay Off-Target:
Kinome-wide selectivity of HM-279 was also assessed in a panel of 255 kinase assays. HM-279 exhibite ...

Potency
Cellular
In Vitro

TGFBR1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.4c02293

In Vivo Validations

Mouse
Dose: 5 mg/Kg
Route of delivery: Intravenous
Plasma half life: 0.59 h
Systemic clearance: 0.32 L/h/kg
Area Under the Curve:: 15796 hr·ng/mL
Volume of Distribution at Steady-State: 0.21 L/Kg

DOI Reference: 10.1021/acs.jmedchem.4c02293

Dose: 30 mg/Kg
Route of delivery: Oral
Plasma half life: 3.36 h
Cmax: 9724 ng/mL
Tmax: 0.5 h
Area Under the Curve:: 41,724 hr·ng/mL
Bioavailability: 44%

DOI Reference: 10.1021/acs.jmedchem.4c02293

Rat
Dose: 1 mg/Kg
Route of delivery: Intravenous
Plasma half life: 0.61 h
Systemic clearance: 1.35 L/h/Kg
Area Under the Curve:: 760 hr·ng/mL
Volume of Distribution at Steady-State: 1.07 L/Kg

DOI Reference: 10.1021/acs.jmedchem.4c02293

Dose: 10 mg/Kg
Route of delivery: Oral
Plasma half life: 0.89 h
Cmax: 2680 ng/mL
Tmax: 1 h
Area Under the Curve:: 6282 hr·ng/mL
Bioavailability: 82.6%

DOI Reference: 10.1021/acs.jmedchem.4c02293

Dog
Dose: 1 mg/Kg
Route of delivery: Intravenous
Plasma half life: 0.29 h
Systemic clearance: 10.7 L/h/Kg
Area Under the Curve:: 96.7 hr·ng/mL
Volume of Distribution at Steady-State: 3.42 L/Kg

DOI Reference: 10.1021/acs.jmedchem.4c02293

Dose: 6.72 mg/Kg
Route of delivery: Oral
Plasma half life: 0.605 h
Cmax: 109 ng/mL
Tmax: 0.82 h
Area Under the Curve:: 163 hr·ng/mL
Bioavailability: 25%

DOI Reference: 10.1021/acs.jmedchem.4c02293

Chemical Information

Molecular Formula C21H23N7O2S
SMILEs CC#CCn1cc(N(c2nc(C(N)=O)c(-c3cc(C(=O)N(C)C)c[nH]3)s2)C2CC2)cn1
InChI InChI=1S/C21H23N7O2S/c1-4-5-8-27-12-15(11-24-27)28(14-6-7-14)21-25-17(19(22)29)18(31-21)16-9-13(10-23-16)20(30)26(2)3/h9-12,14,23H,6-8H2,1-3H3,(H2,22,29)
Molecular weight 437.16 Da
AlogP 2.459200000000001
HBond acceptors 9
HBond donors 3
Atoms 54

References

Publications

Cross References

Expert Reviews

No SERP comments found for HM-279

Probe HM-279 is in the process of SERP review.

Please continue to check back for new reviews and commentary.