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CRT0066101 dihydrochloride

CAS No. : 1883545-60-5

產(chǎn)品活性：CRT0066101 dihydrochloride is a potent and specific PKD inhibitor with IC₅₀ values of 1, 2.5 and 2 nM for PKD1, 2, and 3 respectively.

研究領(lǐng)域：Apoptosis

作用靶點：PKD

In Vitro: CRT0066101 specifically blocks PKD1/2 activity and does not suppress PKCα/PKCβ/PKCε activity in multiple cancer cell types including A549 (lung) and MiaPaCa-2 (pancreas). CRT0066101 significantly inhibits Panc-1 cell proliferation with an IC₅₀ value of 1 µM. Treatment with CRT0066101 results in a 6-10 fold induction of apoptosis in Panc-1 cells. CRT0066101 significantly reduces cell proliferation of Colo357, Panc-1, MiaPaCa-2, and AsPC-1 cells but has a modest effect in Capan-2 cells. CRT0066101 (5 µM) blocks both the basal and NT-induced pS916-PKD1/2 (activated PKD1/2) in Panc-1 and Panc-28 cells. CRT0066101 reduces PKD-dependent NF-κB activation and NF-κB-dependent gene expressions in Panc-1.

In Vivo: Optimal therapeutic concentrations (8 µM) of CRT0066101 are detectable 6 h after oral administration of this drug. CRT0066101 given orally (80 mg/kg/day) for 28 days significantly abrogates PaCa growth in Panc-1 subcutaneous xenograft model. Activated PKD1/2 expression in the treated tumor-explants is significantly inhibited with peak tumor concentration (12 µM) of CRT0066101 achieved within 2 h after oral administration. Further, CRT0066101 given orally (80 mg/kg/day) for 21 days in Panc-1 orthotopic model potently blocks tumor growth in vivo. CRT0066101 significantly reduces Ki-67⁺ proliferation index, increases TUNEL+ apoptotic cells (p<0.05), and abrogates expression of NF-κB-dependent proteins including cyclin D1, survivin, and cIAP-1.

相關(guān)產(chǎn)品：Bioactive Compound Library Plus  |  Apoptosis Compound Library  |  Kinase Inhibitor Library  |  Anti-Cancer Compound Library  |  Targeted Diversity Library  |  Heterocyclic Compound Library  |  Membrane Protein-targeted Compound Library  |  CID755673  |  kb NB 142-70  |  CID 2011756  |  CRT5  |  3-IN-PP1  |  PKD-IN-1  |  BPKDi  |  Protein kinase D inhibitor 1

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