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1877286-69-5

1877286-69-5 structure
1877286-69-5 structure
  • Name: Dual BET-Kinase inhibitor 3
  • Chemical Name: Dual BET-Kinase inhibitor 3
  • CAS Number: 1877286-69-5
  • Molecular Formula: C26H34FN7O2S
  • Molecular Weight: 527.663
  • Create Date: 2020-01-11 17:31:52
  • Modify Date: 2024-05-01 19:19:45
  • 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; also significantly inhibits NTRK3 (IC50=5 nM), ROS1 (IC50=11 nM), PDGFRβ (IC50=16 nM) and FGFR1 (IC50=43 nM), shows equal activity against the first and second bromodomains of BRD4 and shows only slightly reduced activity against BRDT-1; 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.

Name Dual BET-Kinase inhibitor 3
Description 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; also significantly inhibits NTRK3 (IC50=5 nM), ROS1 (IC50=11 nM), PDGFRβ (IC50=16 nM) and FGFR1 (IC50=43 nM), shows equal activity against the first and second bromodomains of BRD4 and shows only slightly reduced activity against BRDT-1; 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.
References References 1. Ember SW, et al. Mol Cancer Ther. 2017 Jun;16(6):1054-1067. View Related Products by Target Bromodomain
Molecular Formula C26H34FN7O2S
Molecular Weight 527.663
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