BPR1J-340 is a potent and selective FLT3 inhibitor with potential anticancer activity. BPR1J-340 was identified as a potent FLT3 inhibitor by bioactive compound kinase activity (IC50 approximately 25 nM) and cellular proliferation (GC50 approximately 5 nM) assays. BPR1J-340 inhibited the phosphorylation of FLT3 and STAT5 and triggered apoptosis in FLT3-ITD(+) AML cells. The pharmacokinetic parameters of BPR1J-340 in rats were determined. BPR1J-340 also demonstrated pronounced tumor growth inhibition and regression in FLT3-ITD(+) AML murine xenograft models. The combination treatment of the HDAC inhibitor vorinostat (SAHA) with BPR1J-340 synergistically induced apoptosis via Mcl-1 down-regulation in MOLM-13 AML cells, indicating that the combination of selective FLT3 kinase inhibitors and HDAC inhibitors could exhibit clinical benefit in AML therapy. References: Lin WH, Yeh TK, Jiaang WT, Yen KJ, Chen CH, Huang CT, Yen SC, Hsieh SY, Chou LH, Chen CP, Chiu CH, Kao LC, Chao YS, Chen CT, Hsu JT. Evaluation of the antitumor effects of BPR1J-340, a potent and selective FLT3 inhibitor, alone or in combination with an HDAC inhibitor, vorinostat, in AML cancer. PLoS One. 2014 Jan 8;9(1):e83160. doi: 10.1371/journal.pone.0083160. eCollection 2014. PubMed PMID: 24416160; PubMed Central PMCID: PMC3885398

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CAS：1395051-72-5