DCLK1-IN-1

SKU: orb1298950

Description

DCLK1-IN-1 is a potent and selective chemical probe for DCLK1/2 kinase inhibition, with IC50 values in the low nanomolar range. This in vivo-compatible tool compound enables the investigation of DCLK1 biology and its functional roles in cancer models, both in vitro and in vivo.

Research Area

Signal Transduction

Key Properties

• CAS Number: 2222635-15-4
• MW: 527.54
• Purity: >99.99% (May vary between batches)
• Formula: C₂₆H₂₈F₃N₇O₂
• SMILES: COc1cc(ccc1Nc1ncc2N(CC(F)(F)F)C(=O)c3ccccc3N(C)c2n1)N1CCN(C)CC1
• Target: Others
• Solubility: 2% DMSO+40% PEG300+5% Tween 80+53% Saline:1 mg/mL (1.9 mM);DMSO:11.9 mg/mL (22.56 mM)

Bioactivity

• In Vivo:
  DCLK1-IN-1 (3 mg/kg, intravenous injection; 10 mg/kg, oral administration) has good pharmacokinetic characteristics in mice, with a half-life of 2.09 hours, an area under the curve (AUCinf) of 5506 hr*ng/mL, and an oral bioavailability of 81%.
  Read more...
• In Vitro:
  METHODS: A NanoBRET tracer (TAE684-NanoBRET-590) was synthesized and a DCLK1 NanoBRET assay was developed to measure the effect of DCLK1-IN-1 on cell proliferation in HCT116 cells. RESULTS The IC50 value of DCLK1-IN-1 against HCT116 cells was 279nM. METHODS: ACHN, 786-O, and CAKI-1 RCC cells were treated with DCLK1-IN-1 (0.5, 1, 5, 10 μM) and subjected to wound healing assays. RESULTS DCLK1-IN-1 exerted a significant anti-migratory effect on ACHN, 786-O, and CAKI-1 RCC cells, with ACHN and CAKI-1 cells showing a typical dose-dependent decrease in wound healing from 0.5 to 10 μM, while 786-O cells showed a significant decrease at a dose of 10 μM.
  Read more...

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

cancer, DCLK1IN1, DCLK-1-IN-1, DCLK1-IN-1, DCLK1 IN 1, PDAC, KRAS, inhibit, low, ERK, Inhibitor, toxicity, signaling, selective

Compound Identifiers

PubChem CID

134457640