BPR1J-097
BPR1J-097 is a novel small molecule FLT-3 inhibitor with promising in vivo anti-tumour activities. BPR1J-097 may be useful in AML treatments.IC50 of BPR1J-097 required to inhibit FLT3 kinase activity ranged from 1 to 10 nM, and the 50% growth inhibition concentrations (GC(50)s) were 21±7 and 46±14 nM for MOLM-13 and MV4-11 cells, respectively. BPR1J-097 inhibited FLT3/signal transducer and activator of transcription 5 phosphorylation and triggered apoptosis in FLT3-driven AML cells. BPR1J-097 also showed favourable pharmacokinetic property and pronounced dose-dependent tumour growth inhibition and regression in FLT3-driven AML murine xenograft models.
1: Lin WH, Jiaang WT, Chen CW, Yen KJ, Hsieh SY, Yen SC, Chen CP, Chang KY, Chang CY, Chang TY, Huang YL, Yeh TK, Chao YS, Chen CT, Hsu JT. BPR1J-097, a novel FLT3 kinase inhibitor, exerts potent inhibitory activity against AML. Br J Cancer. 2012 Jan 31;106(3):475-81. doi: 10.1038/bjc.2011.564. Epub 2011 Dec 20. PubMed PMID: 22187040; PubMed Central PMCID: PMC3273346.
| Chemical | |
|---|---|
| CAS Num | 1327167-19-0 |
| Chemical Formula | C27H28N6O3S |
| Molecular Weight | 516.61 |
| IUPAC Chemical Name | 4-(4-methylpiperazin-1-yl)-N-(3-(3-(phenylsulfonamido)phenyl)-1H-pyrazol-5-yl)benzamide. |
| Exact Mass | 516.19436 |
| Elemental Analysis | C, 62.77; H, 5.46; N, 16.27; O, 9.29; S, 6.21 |
| Synonym | BPR1J097; BPR1J-097; BPR1J 097; BPR1-J097; BPR1 J097; BPR1J097 |
| Solubility | Soluble in DMSO, not in water |
| SMILES Code | O=C(NC1=CC(C2=CC=CC(NS(=O)(C3=CC=CC=C3)=O)=C2)=NN1)C4=CC=C(N5CCN(C)CC5)C=C4 |
| Biological | |
| Targets and Effects | N/A |
| Pathways | Apoptosis |
| Physical | |
| Appearance | white solid powder |
| Purity | >98% (or refer to the Certificate of Analysis) |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shelf Life | >5 years if stored properly |
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