Home Protein Tyrosine Kinase Trk receptor inhibitor - Tie-2 inhibitor - VEGFR inhibitor - c-Met inhibitor Altiratinib For research use only.

Altiratinib

Synonyms: DCC-2701

Altiratinib (DCC-2701) is a potent single-digit nanomolar inhibitor of TRK, Met (c-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 (c-Met) and Met (c-Met) mutant with IC50 values in the range of 0.3-6 nM.

Altiratinib Chemical Structure

Altiratinib Chemical Structure

CAS: 1345847-93-9

Selleck's Altiratinib has been cited by 2 publications

Purity & Quality Control

Batch: S641201 DMSO] 100 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.82%
99.82

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Biological Activity

Description Altiratinib (DCC-2701) is a potent single-digit nanomolar inhibitor of TRK, Met (c-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 (c-Met) and Met (c-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)		 Click to View More Targets
0.37 nM 0.85 nM 0.85 nM 1.2 nM 1.3 nM
In vitro
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models MKN-45 xenograft mouse (Female nude mice)
Dosages 10 and 30 mg/kg
Administration oral
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02228811 Terminated Locally Advanced Tumors|Metastatic Solid Tumors|Cancers With MET Genomic Alterations|Cancers With TRK Genomic Alterations Deciphera Pharmaceuticals LLC June 2014 Phase 1

Chemical lnformation & Solubility

Molecular Weight 510.46 Formula

C26H21F3N4O4
CAS No. 1345847-93-9 SDF --
Smiles C1CC1C(=O)NC2=NC=CC(=C2)OC3=C(C=C(C(=C3)F)NC(=O)C4(CC4)C(=O)NC5=CC=C(C=C5)F)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (195.9 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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