Irbinitinib

• CAT Number: I005570
• CAS Number: 937263-43-9
• Molecular Formula: C26H24N8O2
• Molecular Weight: 480.52
• Purity: 98%
• Target: ERBB2
• Target Protein: P04626
• Solubility: 10 mM in DMSO
• Appearance: Solid
• Storage: Dry, dark and at 2 - 8 °C for six months or -20°C for two years.
• IC50: IC50:8 nM(HER2 inhibitor)
• IUPAC Name: 6-N-(4,4-dimethyl-5H-1,3-oxazol-2-yl)-4-N-[3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]quinazoline-4,6-diamine
• InChI: InChI=1S/C26H24N8O2/c1-16-10-17(5-7-22(16)36-19-8-9-34-23(12-19)28-15-30-34)31-24-20-11-18(4-6-21(20)27-14-29-24)32-25-33-26(2,3)13-35-25/h4-12,14-15H,13H2,1-3H3,(H,32,33)(H,27,29,31)
• InChIKey: SDEAXTCZPQIFQM-UHFFFAOYSA-N
• SMILES: CC1=C(C=CC(=C1)NC2=NC=NC3=C2C=C(C=C3)NC4=NC(CO4)(C)C)OC5=CC6=NC=NN6C=C5

Irbinitinib(Cat No.:I005570), also known as TP-0903, is an orally administered small molecule inhibitor of the receptor tyrosine kinase AXL. AXL plays a crucial role in the regulation of various cellular processes such as proliferation, migration, invasion, and survival. Overexpression of AXL has been associated with poor prognosis in various types of cancer. Irbinitinib has shown potent anti-tumor activity in preclinical studies and is being investigated in clinical trials for the treatment of solid tumors, including non-small cell lung cancer and triple-negative breast cancer.

Overview of Clinical Research

Irbinitinib is a ERBB 2 receptor antagonist. It has been granted for the orphan drug status in Colorectal cancer and Breast cancer.

Reference

1.Moulder, Stacy L., et al. "Phase I study of ONT-380, a HER2 inhibitor, in patients with HER2+-advanced solid tumors, with an expansion cohort in HER2+ metastatic breast cancer (MBC)." Clinical Cancer Research 23.14 (2017): 3529-3536.
2.Meric-Bernstam, Funda, et al. "Advances in HER2-targeted therapy: novel agents and opportunities beyond breast and gastric cancer." Clinical Cancer Research 25.7 (2019): 2033-2041.
3.Lee, Patrice, et al. "In vivo activity of ARRY-380, a potent, small Molecule inhibitor of ErbB2 in combination with trastuzumab, docetaxel or bevacizumab." (2009): 5104-5104.