Cas No.: | 364042-47-7 |
Chemical Name: | 7-[Trans-4-(4-methyl-1-piperazinyl)cyclohexyl]-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine trihydrochloride |
Synonyms: | A-419259 trihydrochloride; A419259; A 419259. |
SMILES: | C1=NC(N)=C2C(C3=CC=C(OC4=CC=CC=C4)C=C3)=CN([C@H]3CC[C@H](N4CCC(C)CC4)CC3)C2=N1 |
Formula: | C29H37Cl3N6O |
M.Wt: | 592.006 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | RK-20449 (RK20449) is a potent, small molecule inhibitor of hematopoietic cell kinase (HCK) with IC50 of 0.43 nM; displays an IC50 <100 nM against 7 kinases in a panel of 107 human kinases, all of which are SFKs (FYN, HCK, LCK, LYNa, LYNb, SRC, and YES), consistent with the high level of amino acid sequence homology among the SFKs. potently inhibits CD34+ CD38− human primary AML cell proliferation to a greater extent than the known SFK inhibitor PP2, shows dose-dependent inhibition of leukemia stem cells (LSCs) proliferation with IC50 <1 uM in 17 of 25 AML cases; significantly reduces human LSC and non-stem AML burden in vivo models. |