- Altiratinib
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- $48.00
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2026-08-20
- CAS:1345847-93-9
- Purity: 99.75%
- Supply Ability: 10g
- Altiratinib
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- $1.00
-
2019-09-06
- CAS:1345847-93-9
- Min. Order: 1KG
- Purity: 98%
- Supply Ability: 20kg
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| | Altiratinib Basic information |
| Product Name: | Altiratinib | | Synonyms: | N-(4-(2-(cyclopropanecarboxamido)pyridin-4-yloxy)-2,5-difluorophenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide;Altiratinib(DCC2701);Altiratinib;DP 5164;DCC2701
(Altiratinib);DCC-2701;Altiratinib(DCC-22701);Altiratinib(DCC2701,DP5164) | | CAS: | 1345847-93-9 | | MF: | C26H21F3N4O4 | | MW: | 510.47 | | EINECS: | 1592732-453-0 | | Product Categories: | Inhibitors | | Mol File: | 1345847-93-9.mol |  |
| | Altiratinib Chemical Properties |
| Boiling point | 763.5±60.0 °C(Predicted) | | density | 1.557±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | ≥21.55 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH | | form | solid | | pka | 12.09±0.70(Predicted) | | color | Light yellow to khaki |
| | Altiratinib Usage And Synthesis |
| Uses | Altiratinib (DCC-2701) is a multi-targeted kinase inhibitor with IC50s of 2.7, 8, 9.2, 9.3, 0.85, 4.6, 0.83 nM for MET, TIE2, VEGFR2, FLT3, Trk1, Trk2, and Trk3 respectively. | | Biological Activity | altiratinib (dcc-2701) is a potent inhibitor of c-met/tie-2/vegfr with ic50 values of 2.7, 8.0 and 9.2 nm, respectively [1].hepatocyte growth factor receptor (c-met) is a tyrosine kinase receptor for hepatocyte growth factor and is essential for wound healing and embryonic development. tek tyrosine kinase (tie-2) is a receptor for angiopoietin-1 (ang-1) and is important for endothelial cell-smooth muscle cell communication. vegfr is a tyrosine kinase receptor for vascular endothelial growth factor that involved in both vasculogenesis and angiogenesis.altiratinib (dcc-2701) is a potent c-met/tie-2/vegfr inhibitor. altiratinib potently inhibited met kinase and activating oncogenic met mutations and also inhibited trka, trkb and trkc kinases with ic50 values of 0.85, 4.6, and 0.83 nm, respectively. in ebc-1 nsclc and mkn-45 gastric cancer cell lines overexpressing met, altiratinib inhibited met phosphorylation with ic50 values of 0.85 and 2.2 nm, respectively. in vegf-stimulated huvecs, altiratinib inhibited vegfr2 phosphorylation with ic50 value of 4.7 nm. in huvecs and ea.hy926 cells, altiratinib inhibited tie2 phosphorylation stimulated by ang-1 with ic50 values of 1.0 and 2.6 nm, respectively [1].in the met-amplified mkn-45 xenograft model, altiratinib (30 mg/kg) inhibited met phosphorylation by >95% for the 24-hour period [1]. in nude mouse xenografted skov3 cells, dcc-2701 (10 or 20 mg/kg for 28 days) significantly reduced tumor burden by 53% and 52%, respectively [2]. | | in vivo | A single oral dose of 30 mg/kg Altiratinib leads to >95% inhibition of MET phosphorylation for the entire 24-hour period. A single 10 mg/kg oral dose of Altiratinib exhibits complete inhibition of MET phosphorylation through 12 hours and 73% inhibition at 24 hours postdose. Altiratinib dosed at 10 mg/kg twice a day leads to a significant 90% decrease in BLI signal. 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[1]. | | IC 50 | VEGFR2: 9.2 nM (IC50); Trk1: 0.85 nM (IC50); Trk2: 4.6 nM (IC50); Trk3: 0.93 nM (IC50); MET: 2.7 nM (IC50); TIE2: 8 nM (IC50); FLT3: 9.3 nM (IC50) | | references | [1]. smith bd, kaufman md, leary cb, et al. altiratinib inhibits tumor growth, invasion, angiogenesis, and microenvironment-mediated drug resistance via balanced inhibition of met, tie2, and vegfr2. mol cancer ther, 2015.
[2]. kwon y, smith bd, zhou y, et al. effective inhibition of c-met-mediated signaling, growth and migration of ovarian cancer cells is influenced by the ovarian tissue microenvironment. oncogene, 2015, 34(2): 144-153. |
| | Altiratinib Preparation Products And Raw materials |
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