BPR1J-097
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 401161

CAS#: 1327167-19-0

Description: 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.


Price and Availability

Size
Price

5mg
USD 90
50mg
USD 450
500mg
USD 1650
Size
Price

10mg
USD 150
100mg
USD 650
1g
USD 2750
Size
Price

25mg
USD 250
200mg
USD 950
2g
Ask price

BPR1J-097, purity > 98%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 1g may be 2 weeks.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 401161
Name: BPR1J-097
CAS#: 1327167-19-0
Chemical Formula: C27H28N6O3S
Exact Mass: 516.19436
Molecular Weight: 516.61
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

IUPAC/Chemical Name: 4-(4-methylpiperazin-1-yl)-N-(3-(3-(phenylsulfonamido)phenyl)-1H-pyrazol-5-yl)benzamide.

InChi Key: RRKKHABFIOHAOI-UHFFFAOYSA-N

InChi Code: InChI=1S/C27H28N6O3S/c1-32-14-16-33(17-15-32)23-12-10-20(11-13-23)27(34)28-26-19-25(29-30-26)21-6-5-7-22(18-21)31-37(35,36)24-8-3-2-4-9-24/h2-13,18-19,31H,14-17H2,1H3,(H2,28,29,30,34)

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


Technical Data

Appearance:
white solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (MSDS):

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).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>5 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

BPR1J-097 was discovered by a rational design strategy. BPR1J-097 with a novel sulphonamide pharmacophore exhibits potent FLT3-inhibitory activity and has potent growth-inhibitory effects on FLT3-ITD leukaemic cells. According to our SAR studies, It was found that sulphonamide pharmacophore preferred at meta-position of the phenyl ring, and that replacement the sulphonamide group of BPR1J-097 with the urea group resulted in a significant loss in cellular potency. Inhibition of FLT3 resulted in blockage of FLT3 and STAT5 phosphorylation and triggered apoptosis in cancer cells relying on FLT3 signalling for survival. In addition, BPR1J-097 showed  favourable pharmacokinetic properties and significant  dose dependent tumour reduction in FLT3-ITD murine xenograft models. These results demonstrate the potential of BPR1J-097 as a therapeutic candidate for treatment of AML patients. Further preclinical and clinical studies in AML patients are warranted. (source: Br J Cancer. 2012 Jan 31;106(3):475-81. doi: 10.1038/bjc.2011.564. Epub 2011 Dec 20.).
  
  


References

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.