RGNCY-0049 (RK-20449 HCK inhibitor)

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RK-20449 is a pyrrolo-pyrimidine derivative HCK inhibitor.  Crystal structure analysis demonstrated that RK-20449 bound the activation pocket of HCK.  In vivo administration of Rk-20449 to non-obese (NOD)/severe combined immunodeficient (SCIS)/IL2rg(null) mice engrafted with aggressive therapy resistant AML, resulted in a significant reduction in human LSC and non-stem AML burden.  RK-20449 may eliminate chemotherapy resistant LSCs and prevent relapse, and thereby improve patient outcomes. HCK inhibition IC50 of 0.43 nM.


Systematic Name: 7-((1r,4r)-4-(4-methylpiperazin-1-yl)cyclohexyl)-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine 

Molecular Weight: 482.63 

Formula: C29H34N6

PMID: 23596204

Tags: Small molecules, RK-20449, AML, RGNCY-0049, RK20449, immunodeficiency