l General Information |
Product Name | Gandotinib (LY2784544) |
General description | Gandotinib (LY2784544) is a potent JAK2 inhibitor. |
Synonym | 3-[(4-chloro-2-fluorophenyl)methyl]-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(morpholin-4-ylmethyl)imidazo[1,2-b]pyridazin-6-amine |
Purity | ≥98.0%(HPLC) | CAS Number | 1229236-86-5 |
Formula | C23H25ClFN7O | Molecular Weight | 469.949 |
Suitability | BioReagent, suitable for cell culture, etc. |
l Physical and Chemical Information |
Appearance | solid |
Solubility(25℃) | DMSO | ≥50mg/mL |
Ethanol | ≥5mg/mL |
Water | Insoluble |
l Biological Information |
Biochem/Physiol
Actions | Gandotinib is an orally bioavailable imidazopyridazine and inhibitor of Janus kinase 2 mutant V617F (JAK2V617F), with potential antineoplastic activity. Upon oral administration, gandotinib selectively and competitively inhibits the activation of JAK2V617F, which may result in the inhibition of the JAK-STAT signaling pathway and the induction of apoptosis in JAK2V617F-expressing tumor cells. JAK2V617F has a substitution of phenylalanine for valine at amino acid position 617 and plays a key role in tumor cell proliferation and survival. Gandotinib (LY2784544) is a potent JAK2 inhibitor with IC50 of 3 nM, effective in JAK2V617F, 8- and 20-fold selective versus JAK1 and JAK3. |
Application | Gandotinib has been used in trials studying the treatment of Myelofibrosis, Polycythemia Vera, Primary Myelofibrosis, Thrombocythemia, Essential, and Myeloproliferative Disorders, among others. |
l Storage |
Storage temp. | -20℃ |
l Precautions and Disclaimer |
This product is for R&D use only, not for drug, household, or other uses. |
l References |
1. http://www.drugbank.ca 2. https://ncit.nci.nih.gov 3. https://www.ncbi.nlm.nih.gov |
