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Chemical Structure : BPR1J373
Catalog No.: PC-35619Not For Human Use, Lab Use Only.
BPR1J373 is a potent, orally available multitargeted kinase inhibitor, potently inhibits FLT3, c-KIT, VEGFR1-3, Aurora A, PDGFRα, PDGFRβ, RET, and SRC with IC50 values of <100 nM.
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BPR1J373 is a potent, orally available multitargeted kinase inhibitor, potently inhibits FLT3, c-KIT, VEGFR1-3, Aurora A, PDGFRα, PDGFRβ, RET, and SRC with IC50 values of <100 nM.
BPR1J373 inhibits cell proliferation of myeloid leukemia cell lines and primary leukemia cells with constitutively activated c-KIT (KG-1, K562 cell with IC50 of 45 and 49 nM).
BPR1J373also suppresses c-KIT in AML cell lines and primary AML cells; induces apoptosis by mitochondrial intrinsic pathway through upregulation of proapoptotic proteins Bax and Bak and caspase 8 and 9 activation in Kasumi-1 cells, induces cell-cycle arrest for c-KIT–driven leukemia cells via targeting different signals.
BPR1J373 effectively suppressed Kasumi-1 cells in xenograft mouse model, effectively suppresses c-KIT phosphorylation of D816V mutation.
| M.Wt | 549.65 | |
| Formula | C26H31N9O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Chen LT, et al. Mol Cancer Ther. 2016 Oct;15(10):2323-2333.
2. Tsai HJ, et al. Cancer Sci. 2018 Aug 24. doi: 10.1111/cas.13773.
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