Altiratinib

Catalog No.S6412 Synonyms: DCC-2701

Altiratinib Chemical Structure

Molecular Weight(MW): 510.46

Altiratinib is a potent single-digit nanomolar inhibitor of TRK, MET, TIE2, and VEGFR2 kinases with IC50 vaules of 0.9 nM, 4.6 nM, and 0.8 nM for TRKA, B, and C, respectively. It inhibits MET and MET mutant with IC50 values in the range of 0.3-6 nM.

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Biological Activity

Description Altiratinib is a potent single-digit nanomolar inhibitor of TRK, MET, TIE2, and VEGFR2 kinases with IC50 vaules of 0.9 nM, 4.6 nM, and 0.8 nM for TRKA, B, and C, respectively. It inhibits MET and MET mutant with IC50 values in the range of 0.3-6 nM.
Targets
MET Y1230C [1]
(Cell-free assay)
TrkA [1]
(Cell-free assay)
TrkC [1]
(Cell-free assay)
MET Y1230C [1]
(Cell-free assay)
MET D1228N [1]
(Cell-free assay)
0.37 nM 0.85 nM 0.85 nM 1.2 nM 1.3 nM
In vitro

Altiratinib is >10-fold selective for MET versus FMS and KIT, and >50-fold selective for MET versus ABL1, FYN, HER1 (EGFR), p38α (MAPK14), PDGFRα, PDGFRβ, RET, and SRC. Altiratinib exhibits IC50s of 0.69 nmol/L in K562 cells, 1.2 nmol/L in SK-N-SH cells for inhibition of NGF-stimulated TRKA phosphorylation. Altiratinib inhibits constitutive TRKA phosphorylation with an IC50 of 1.4 nmol/L in KM-12 cells. Altiratinib inhibits HGF-stimulated MET phosphorylation in HUVECs, exhibiting an IC50 of 2.3 nmol/L. In ANG1-stimulated HUVECs and EA.hy926 cells, altiratinib exhibits IC50 values of 1.0 nmol/L and 2.6 nmol/L, respectively, for inhibition of TIE2 phosphorylation. In VEGF-stimulated HUVECs, altiratinib inhibits VEGFR2 phosphorylation with an IC50 of 4.7 nmol/L. Altiratinib potently inhibits cellular proliferation in MET-amplified EBC-1 and MKN-45 cells, as well as TPM3-TRKA fusion KM-12 cells, but only weakly inhibits other cancer cell lines, including proliferation of M-NFS-60 (IC50, 770 nmol/L); A375, BT-474, HCT-116, PC-3, SK-MEL-28, U87, and A549 cells (IC50s > 1,000 nmol/L)[1].

In vivo

Altiratinib alone and in combination with bevacizumab increases survival and decreases circulating TIE2+-expressing monocytes in the U87 glioma model. In the PyMT syngeneic mammary tumor model which recapitulates many features of human breast cancer, altiratinib alone and in combination with paclitaxel inhibits PyMT mammary tumor growth, reduces tumoral TIE2+ stromal cell density, and inhibits lung metastasis. Altiratinib achieves a brain:plasma ratio of 0.23 after systemic dosing, indicating significant penetration of the murine blood-brain barrier[1].

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: EBC-1, M-NFS-60, SK-MEL-28, MKN-45, MV-4-11, A375, HCT-116, BT-474, KM-12, PC-3, and U-87-MG cells
  • Concentrations: --
  • Incubation Time: 72 h
  • Method:

    Cells are added to 96-well (EBC-1, M-NFS-60, and SK-MEL-28: 2,500 cells/well; MKN-45: 5,000 cells/well; MV-4-11: 10,000 cells/well) or 384-well plates (A375 and HCT-116: 625 cells/well; BT-474, KM-12, PC-3, and U-87-MG: 1,250 cells/well). Plates are incubated for 72 hours. Viable cells are quantified using resazurin using a plate reader with excitation at 540 nm and emission at 600 nm.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: MKN-45 xenograft mouse (Female nude mice)
  • Formulation: 0.4% HMPC
  • Dosages: 10 and 30 mg/kg
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (195.9 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 510.46
Formula

C26H21F3N4O4

CAS No. 1345847-93-9
Storage powder
in solvent
Synonyms DCC-2701

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Trk receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID