UNC-2025 ( UNC2025, UNC2025, UNC 2025 )

Catalog No. M17294 CAS No. 1429881-91-3

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Product Name

UNC-2025
Note

Research use only, not for human use.
Brief Description

UNC-2025（ IC50 of 0.74 nM and 0.8 nM） is a potent and orally bioavailable dual MER/FLT3 inhibitor. UNC-2025 is about 20-fold selectivity higher than Axl and Tyro3.
Description

UNC-2025 is a novel potent and highly orally bioavailable Mer/FLT3 dual inhibitor, 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 profiling versus more than 300 kinases in vitro and cellular selectivity assessments demonstrate that UNC-2025 has similar subnanomolar activity against Flt3, an additional important target in acute myelogenous leukemia (AML), with pharmacologically useful selectivity versus other kinases examined.
Synonyms

UNC2025, UNC2025, UNC 2025
Pathway

Membrane Transporter/Ion Channel
Target

TRP/TRPV Channel
Recptor

FLT3; AXL; Mer; Tyro3
Research Area

Cancer
Indication

——

CAS Number

1429881-91-3
Formula Weight

513.12
Molecular Formula

C28H41ClN6O
Purity

98%
Solubility

DMSO : 33.33 mg/mL. 69.92 mM;
SMILES

CCCCNc1ncc2c(cn(c2n1)[C@H]1CC[C@@H](CC1)O)c1ccc(cc1)CN1CCN(CC1)C.Cl.Cl
Chemical Name

(1r,4r)-4-(2-(butylamino)-5-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclohexanol

1. Zhang W, et al. J Med Chem. 2014, 57(16), 7031-7041.

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