ALTIRATINIB (DCC-2701)
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| Catalog No. | APIM050074 |
|---|---|
| Product Name | ALTIRATINIB (DCC-2701) |
Description
Background Information:
Abstract (Ref 1): Altiratinib (DCC-2701) was designed based on the rationale of engineering a single therapeutic agent able to address multiple hallmarks of cancer. Specifically, Altiratinib inhibits not only mechanisms of tumor initiation and progression, but also drug resistance mechanisms in the tumor and microenvironment through balanced inhibition of MET, TIE2 (TEK), and VEGFR2 (KDR) kinases. This profile was achieved by optimizing binding into the switch control pocket of all three kinases, inducing type II inactive conformations. Altiratinib durably inhibits MET, both wild-type and mutated forms, in vitro and in vivo. Through its balanced inhibitory potency versus MET, TIE2, and VEGFR2, Altiratinib provides an agent that inhibits three major evasive (re)vascularization and resistance pathways (HGF, ANG, and VEGF) and blocks tumor invasion and metastasis. 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.
Reference:
1. B.D. Smith, 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 Sep;14(9):2023-34. doi: 10.1158/1535-7163.MCT-14-1105. Epub 2015 Aug 18.
2. Proceedings: AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA.
APIM050074: ALTIRATINIB (DCC-2701)
CAS No.: 1345847-93-9.
Molecular Formula: C??H??F?N?O?.
Molecular Weight: 510.5 (or refer to Certificate, batch-specific).
Purity: >99.5% by HPLC.
QC: HPLC-MS, NMR and Elemental Analysis.
Solubility: Refer to Certificate of Analysis.
Storage: Refer to Certificate of Analysis.
