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Chemical Structure : Dual BET-Kinase inhibitor 3
Catalog No.: PC-60930Not For Human Use, Lab Use Only.
Dual BET-Kinase inhibitor 3 is a potent, dual BET bromodomain-kinase inhibitor with IC50 of 34, 1.1 and 1.1 nM for BRD4 BD1, JAK2 and FLT-3, respectively.
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Dual BET-Kinase inhibitor 3 is a potent, dual BET bromodomain-kinase inhibitor with IC50 of 34, 1.1 and 1.1 nM for BRD4 BD1, JAK2 and FLT-3, respectively.
Dual BET-Kinase inhibitor 3 also significantly inhibits NTRK3 (IC50=5 nM), ROS1 (IC50=11 nM), PDGFRβ (IC50=16 nM) and FGFR1 (IC50=43 nM).
Dual BET-Kinase inhibitor 3 shows equal activity against the first and second bromodomains of BRD4 and shows only slightly reduced activity against BRDT-1.
Dual BET-Kinase inhibitor 3 inhibits cell growth of MM and AML cell lines with IC50 of <1 uM, reduces c-MYC and p-STAT3 levels and induces G1 arrest, display differential activity across cancer cell lineages.
| M.Wt | 527.663 | |
| Formula | C26H34FN7O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Ember SW, et al. Mol Cancer Ther. 2017 Jun;16(6):1054-1067.
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