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Dclk1-IN-1

  Cat. No.:  DC58110   Featured
Chemical Structure
2222635-15-4
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Field of application
DCLK1-IN-1 is a selective, oral bioavailability in vivo-compatible chemical probe of the doublecortin like kinase 1 (DCLK1 kinase) domain. DCLK1-IN-1 inhibits DCLK1 and DCLK2 kinases (IC50: DCLK1=9.5/57.2 nM and DCLK2=31/103 nM in binding and kinase assay, respectively). DCLK1-IN-1 shows low toxicity, and can investigate DCLK1 biology and establish its role in cancer, like DCLK1+ pancreatic ductal adenocarcinoma (PDAC)[1].
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2222635-15-4
Chemical Name: Dclk1-IN-1
SMILES: FC(C([H])([H])N1C(C2=C([H])C([H])=C([H])C([H])=C2N(C([H])([H])[H])C2C1=C([H])N=C(N=2)N([H])C1C([H])=C([H])C(=C([H])C=1OC([H])([H])[H])N1C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])C1([H])[H])=O)(F)F
Formula: C26N7O2F3H28
M.Wt: 527.5414
Purity: >98%
Sotrage: -20
In Vivo: DCLK1-IN-1 has a favorable pharmacokinetic profile in mice, with a half-life of 2.09 hours, an area under the curve of 5,506 h/ng ml and 81% oral bioavailability[1].
In Vitro: DCLK1-IN-1 shows no significant activity against ERK5, ACK, and LRRK2. DCLK1-IN-1 potently binds DCLK1 in HCT116 cells (IC50 = 279 nM). DCLK1-IN-1 significantly inhibited DCLK1, and weakly inhibited ERK5, in PATU-8988T cell lysates and live cells[1].
References: [1]. Ferguson FM, et al. Discovery of a selective inhibitor of doublecortin like kinase 1. Nat Chem Biol. 2020 Apr 6.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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