Ceritinib

Inhibitor of ALK

Structure

SERP Rating

Probe Ceritinib is in the process of SERP review.

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Information

Inhibitor

up to 1 uM

Probe Availability:

In Vitro Validations

Uniprot ID: Q9UM73

Target Class: Kinase

Target SubClass: RTK

Potency: IC50

Potency Value: 0.2 nM

Potency Assay: Enzymatic Inhibition assay (LabChip mobility-shift assay)

PDB ID for probe-target interaction (3D structure): 4MKC

Structure-activity relationship: yes

Target aliases:

ALK tyrosine kinase receptor, ALK, ALK_HUMAN, Anap ...

DOI Reference: 10.1021/jm400402q

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency end-point : IC50 FLT3 60 nM, FGFR2 260 nM, RET 400 nM, FGFR3 430 nM

Potency assay (off target): Enzymatic Inhibition assay (LabChip mobility-shift assay)

Probe Selectivity in Vitro:

Enzymatic Kinase Profile in uM: ABL 1.25, FGFR4 0.95, LYN 0.84, AKT >10, FLT3 0.06, cMET 3.17, GSK3β >10, MKNK2 2.24, Aurora 0.66, IGF-1R 0.008, PAK2 >10, BTK 3.36, InsR 0.007, PDGFRα 1.14, CDK2 3.97, JAK1 3.73, RET 0.4, CDK4 4.72, JAK2 0.61, ROCK2 1.27, EGFR 0.9, JAK3 7.92, SYK 3.05, FGFR2 0.26, cKit 1.28, STK22D 0.023, FGFR3 0.43, LCK 0.56, ZAP70 9.7

Potency assay, off target (cells): Cell Proliferation Assay (Bright-Glo luciferase assay)

Probe Selectivity in Cell:

Cellular Kinase Profile in Ba/F3 Cells (IC50, uM): Tel-ALK 40.7 ± 5.3, Tel-JAK2, 2160 ± 320, Tel-RET, 2304 ± 459, EML4-ALK 2.2 ± 0.5, Tel-KDR, 4210 ± 170, Tel-Ros 141.8 ± 22.7, Tel-FGFR3 >10000, Tel-ckit 2855 ± 215, Tel-Src 1694 ± 276, Tel-FGR 1947 ± 433, Tel-Lck 672 ± 264, Tel-TRKA 2727 ± 222 Tel-FLT3 3143 ± 933, Tel-LYN 2306 ± 552, Tel-TRKB 1829 ± 80, Tel-IGF-1R 410 ± 10, Tel-Met 1339 ± 74, Tel-WT 3250 ± 710

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SERP ratings and comments

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