Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C26H21F3N4O4 |
| Molecular Weight | 510.4645 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
FC1=CC=C(NC(=O)C2(CC2)C(=O)NC3=CC(F)=C(OC4=CC=NC(NC(=O)C5CC5)=C4)C=C3F)C=C1
InChI
InChIKey=GNNDEPIMDAZHRQ-UHFFFAOYSA-N
InChI=1S/C26H21F3N4O4/c27-15-3-5-16(6-4-15)31-24(35)26(8-9-26)25(36)32-20-12-19(29)21(13-18(20)28)37-17-7-10-30-22(11-17)33-23(34)14-1-2-14/h3-7,10-14H,1-2,8-9H2,(H,31,35)(H,32,36)(H,30,33,34)
| Molecular Formula | C26H21F3N4O4 |
| Molecular Weight | 510.4645 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
Altiratinib, a novel c-MET/TIE-2/VEGFR inhibitor, was able to effectively reduce tumor burden in vivo and block c-MET signaling, cell growth and migration. Altiratinib inhibits not only mechanisms of tumor initiation and progression, but also drug resistance mechanisms in the tumor and microenvironment. Altiratinib durably inhibits MET, both wild-type and mutated forms, in vitro and in vivo. Altiratinib exhibits properties amenable to oral administration and exhibits substantial blood-brain barrier penetration, an attribute of significance for eventual treatment of brain cancers and brain metastases. It is currently in Phase 1 clinical development for the treatment of solid tumors.
CNS Activity
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL3717 |
2.7 nM [IC50] | ||
Target ID: CHEMBL2815 |
0.85 nM [IC50] | ||
Target ID: CHEMBL5608 |
0.83 nM [IC50] | ||
Target ID: CHEMBL4898 |
4.6 nM [IC50] | ||
Target ID: CHEMBL4128 |
8.0 nM [IC50] | ||
Target ID: CHEMBL279 |
9.2 nM [IC50] | ||
Target ID: CHEMBL1974 |
9.3 nM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
|||
| Primary | Unknown Approved UseUnknown |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
38823 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/26285778 |
10 mg/kg single, oral dose: 10 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
ALTIRATINIB blood | Mus musculus population: UNHEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Novel MET/TIE2/VEGFR2 inhibitor altiratinib inhibits tumor growth and invasiveness in bevacizumab-resistant glioblastoma mouse models. | 2016-09 |
|
| Altiratinib Inhibits Tumor Growth, Invasion, Angiogenesis, and Microenvironment-Mediated Drug Resistance via Balanced Inhibition of MET, TIE2, and VEGFR2. | 2015-09 |
|
| Effective inhibition of c-MET-mediated signaling, growth and migration of ovarian cancer cells is influenced by the ovarian tissue microenvironment. | 2015-01-08 |
Patents
Sample Use Guides
In escalating dose (starting dose 15 mg) twice daily every 12 hours for a 28-day cycle
Route of Administration:
Oral
EBC-1 (NSCLC) and MKN-45 (gastric cancer) human cancer cell lines genomically amplify and overexpress MET with subsequent
ligand-independent MET activation. Altiratinib inhibited MET phosphorylation with IC50 values of 0.85 nmol/L and 2.2 nM/L, respectively. In the U-87 glioblastoma cell line, MET and HGF are both expressed. Altiratinib blocked autocrine activation of MET phosphorylation in these cells (IC50 of 6.2 nM/L).
| Substance Class |
Chemical
Created
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admin
on
Edited
Mon Mar 31 22:57:46 GMT 2025
by
admin
on
Mon Mar 31 22:57:46 GMT 2025
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| Record UNII |
T678746713
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| Record Status |
Validated (UNII)
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FDA ORPHAN DRUG |
441714
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NCI_THESAURUS |
C1967
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NCI_THESAURUS |
C129825
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NCI_THESAURUS |
C1742
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1345847-93-9
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CHEMBL3545365
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C118290
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300000034087
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BC-79
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T678746713
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54576299
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10100
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ACTIVE MOIETY |
