| Identification | Back Directory | [Name]
Cyclohexanol, 4-[5-[4-[(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)methyl]phenyl]-2-[[(1S)-1-methylbutyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-7-yl]-, trans- | [CAS]
1818234-19-3 | [Synonyms]
UNC 4203
Cyclohexanol, 4-[5-[4-[(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)methyl]phenyl]-2-[[(1S)-1-methylbutyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-7-yl]-, trans- | [Molecular Formula]
C30H44N6O | [MOL File]
1818234-19-3.mol | [Molecular Weight]
504.71 |
| Chemical Properties | Back Directory | [Boiling point ]
682.0±65.0 °C(Predicted) | [density ]
1.22±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
14.63±0.40(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Description]
UNC4203 is a potent and selective MERTK Inhibitor. UNC4203 showed IC50 MerTK=2.4 nM (Ki=0.42 nM); IC50 Axl = 80 nM (Ki=40.22 nM); IC50 Tyro3 = 9.1 nM (Ki=3.87 nM). IC50 FLT3 = 39 nM *Ki=16.14 nM). T1/2 = 3.0 h; %F=15. UNC4203 may be a potential candidate for cancer treatment. | [Uses]
UNC4203 is a potent, orally available and highly selective MERTK inhibitor, with IC50s of 1.2 nM, 140 nM, 42 nM and 90 nM for MERTK, AXL, TYRO3 and FLT3, respectively[1]. | [in vivo]
Mice are treated with UNC4203 (compound 24) at a dose of 10 mg/kg administered via oral (po) or iv routes. Under the condition, UNC4203 (compound 24) has 58% oral bioavailability with a 7.8 h half-life, 1.7 L/kg volume of distribution, and 36 mL/min/kg clearance[1].
| [IC 50]
Axl; Tyro3 | [References]
[1] Hongchao Zheng, et al. UNC5293, a potent, orally available and highly MERTK-selective inhibitor. Eur J Med Chem. 2021 Aug 5;220:113534. DOI:10.1016/j.ejmech.2021.113534 |
|
|