UNC-2025

• CAT Number: I001650
• CAS Number: 1429881-91-3
• Molecular Formula: C₂₈H₄₀N₆O
• Molecular Weight: 476.66
• Purity: ≥95%
• Target: FLT3
• Solubility: DMSO: ≥ 5 mg/mL, H2O: ＜ 4.9 mg/mL
• Storage: Desiccate at -20C
• IC50: 0.8/0.74 nM(MER/FLT3)
• InChI: InChI=1S/C28H40N6O/c1-3-4-13-29-28-30-18-25-26(20-34(27(25)31-28)23-9-11-24(35)12-10-23)22-7-5-21(6-8-22)19-33-16-14-32(2)15-17-33/h5-8,18,20,23-24,35H,3-4,9-17,19H2,1-2H3,(H,29,30,31)
• InChIKey: MJSHVHLADKXCML-UHFFFAOYSA-N
• SMILES: CCCCNC1=NC=C2C(=CN(C2=N1)C3CCC(CC3)O)C4=CC=C(C=C4)CN5CCN(CC5)C

UNC2025 is a potent and orally bioavailable Mer/Flt3 dual inhibitor with IC50 of 0.8/0.74 nM for Mer/Flt3.IC50 value: 0.8/0.74 nM(MER/FLT3)Target: Mer/Flt3 inhibitorUNC2025 was capable of inhibiting Mer phosphorylation in vivo, following oral dosing as demonstrated by pharmaco-dynamic (PD) studies examining phospho-Mer in leukemic blasts from mouse bone marrow. Kinome proling versus more than 300 kinases in vitro and cellular selectivity assessments demonstrate that 11 has similar subnanomolar activity against Flt3, an additional important target in acute myelogenous leukemia (AML), with pharmacologically useful selectivity versus other kinases examined.

Reference

1:UNC2025, a MERTK Small-Molecule Inhibitor, Is Therapeutically Effective Alone and in Combination with Methotrexate in Leukemia Models. DeRyckere D, Lee-Sherick AB, Huey MG, Hill AA, Tyner JW, Jacobsen KM, Page LS, Kirkpatrick GG, Eryildiz F, Montgomery SA, Zhang W, Wang X, Frye SV, Earp HS, Graham DK.Clin Cancer Res. 2017 Mar 15;23(6):1481-1492. doi: 10.1158/1078-0432.CCR-16-1330. Epub 2016 Sep 20. PMID: 27649555 2:UNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitor. Zhang W, DeRyckere D, Hunter D, Liu J, Stashko MA, Minson KA, Cummings CT, Lee M, Glaros TG, Newton DL, Sather S, Zhang D, Kireev D, Janzen WP, Earp HS, Graham DK, Frye SV, Wang X.J Med Chem. 2014 Aug 28;57(16):7031-41. doi: 10.1021/jm500749d. Epub 2014 Aug 6. PMID: 25068800 Free PMC Article