DCLK1-IN-1

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Catalog No.: PC0172

Size: 1 mg, 5 mg,10 mg, 25 mg,50 mg, 100 mg, 200 mg, 500 mg

Description

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).

Molecular Weight	527.54
Formula	C26H28F3N7O2
CAS No.	2222635-15-4
Appearance	Solid
Color	Light yellow to yellow
SMILES	O=C1N(CC(F)(F)F)C2=CN=C(NC3=CC=C(N4CCN(C)CC4)C=C3OC)N=C2N(C)C5=CC=CC=C15
Shipping	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
*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.
*In Vivo*	DCLK1-IN-1 has a favorable pharmacokinetic profile in mice, with a half-life of 2.09/h, an area under the curve of 5506h/ng/mL and 81% oral bioavailability.

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