| Identification | Back Directory | [Name]
1-Piperazinecarboxamide, N-(4-acetylphenyl)-4-[5-methyl-2-[[4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]amino]-4-pyrimidinyl]- | [CAS]
3038183-53-5 | [Synonyms]
1-Piperazinecarboxamide, N-(4-acetylphenyl)-4-[5-methyl-2-[[4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]amino]-4-pyrimidinyl]- | [Molecular Formula]
C34H45N9O2 | [MOL File]
3038183-53-5.mol | [Molecular Weight]
611.78 |
| Hazard Information | Back Directory | [Uses]
JAK2/FLT3-IN-3 (11r) is a dual FLT3 and JAK2 inhibitor, with IC50 values of 2.01 nM, 0.51 nM and 104.40 nM for JAK2, FLT3 and JAK3, respectively. JAK2/FLT3-IN-3 (11r) induces apoptosis and possesses antitumor activity[1]. | [in vivo]
JAK2/FLT3-IN-3 (11r) shows moderate absorption (Tmax = 5.33 h), with a peak concentration of 38.7 ng/mL and an AUC of 522 ng h/mL in rats, and an oral bioavailability of 25.2%[1]. | [IC 50]
JAK2: 2.01 nM (IC50); FLT3: 0.51 nM (IC50); JAK3: 104.40 nM (IC50) | [References]
[1] Sicong Xu, et al. 2-Aminopyrimidine derivatives as selective dual inhibitors of JAK2 and FLT3 for the treatment of acute myeloid leukemia. Bioorg Chem. 2023 May:134:106442. DOI:10.1016/j.bioorg.2023.106442 |
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