1429881-91-3 in bul...

1429881-91-3 in bulk supply 1429881-91-3 on hot selling Offer 1429881-91-3 UNC2025
1429881-91-3 in bulk supply 1429881-91-3 on hot selling Offer 1429881-91-3 UNC2025

1429881-91-3 in bulk supply 1429881-91-3 on hot selling Offer 1429881-91-3 UNC2025

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1429881-91-3 in bulk supply 1429881-91-3 on hot selling Offer 1429881-91-3 UNC2025

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1429881-91-3 in bulk supply on hot selling Offer  UNC2025

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.

UNC2025 is a potent, ATP-competitive and highly orally active Mer/Flt3 inhibitor with IC50 values of 0.74 nM and 0.8 nM, respectively. UNC2025 is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 exhibits an excellent PK properties, and can be used for the investigation of acute leukemia.

 

Details:

UNC2025 is a potent, orally bioavailable inhibitor of the tyrosine kinases Mer and Flt3 (IC50s = 0.74 and 0.80 nM, respectively).It less potently inhibits Axl and Tyro3 (IC50s = 14 and 17 nM, respectively) and a panel of related kinases. UNC2025 blocks colony formation of Mer- and Flt3-dependent tumor cell lines and inhibits Mer phosphorylation in bone marrow leukemia cells in vivo. Pharmacokinetic studies suggest that orally administered UNC2025 at 3 mg/kg will suffice to provide 90% inhibition of Mer and Flt3 at 30 min.

 

Identification
Name   trans-4-[2-(Butylamino)-5-[4-[(4-methyl-1-piperazinyl)methyl]phenyl]-7H-pyrrolo[2,3-d]pyrimidin-7-yl]cyclohexanol
Synonyms   UNC 2025
 
Molecular Structure   CAS # 1429881-91-3, trans-4-[2-(Butylamino)-5-[4-[(4-methyl-1-piperazinyl)methyl]phenyl]-7H-pyrrolo[2,3-d]pyrimidin-7-yl]cyclohexanol, UNC 2025
 
Molecular Formula   C28H40N6O
Molecular Weight   476.66
CAS Registry Number   1429881-91-3
 
Properties
 
Solubility   Insuluble (1.3E-3 g/L) (25 ºC), Calc.*
Density   1.24±0.1 g/cm3 (20 ºC 760 Torr), Calc.*
     
* Calculated using Advanced Chemistry Development (ACD/Labs) Software V11.02 (©1994-2015 ACD/Labs)

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