Oncogene Fusion Protein
A small individual group of tyrosine kinase inhibitors is specifically targeting oncogenic fusion proteins. The expression of these proteins is caused by a reciprocal translocation between chromosomes, 9 and 22 in case of the BCR-ABL fusion protein. About 95% of the patients suffering from chronic myelogenous leukaemia show expression of this particular protein, yet it is also found in two other acute forms of leukaemia[1],[2]. Our product line includes both the very first drug registered on the market inhibiting this specific tyrosine kinase (Axon 1394: STI 571 or Imatinib (Novartis)), as well as well-known follow-up inhibitors, being more potent and/or more active against the emerging Gleevec/Glivec resistant BCR-ABL clones that originate from point mutations inside the kinase domain of the Bcr-Abl protein and disrupt the binding site of Imatinib on the tyrosine kinase (e.g. Axon 1392 and Axon 1396 (Dasatinib and Nilotinib resp.)[3]
[1] The molecular genetics ofPhiladelphia chromosome-positive leukemias. Kurzrock, R., Gutterman, J. Talpaz, M. N. Engl. J. Med. 1988, 319, 990-998.
[2] Dasatinib in imatinib-resistantPhiladelphia chromosome-positive leukemias. Talpaz M, Shah NP, Kantarjian H, et al. N. Engl. J. Med. 2006, 354 2531–2541.
[3] BCR-ABL tyrosine kinase inhibitors in the treatment ofPhiladelphia chromosome positive chronic myeloid leukemia: a review. An, X.; Tiwari, A.; Sun, Y.; Ding, P.; Ashby Jr, C.; Chen, Z. Leukemia research 2010, 34, 1255–1268.
| Axon ID | Name | Description | From price | |
|---|---|---|---|---|
| 2368 | Amuvatinib | RTK inhibitor which effectively inhibits PDGFR, c-Kit and c-Met | €105.00 | |
| 1857 | AP 24534 | BCR-ABL kinase inhibitor (including T315I mutation) | €70.00 | |
| 2757 | Asciminib | Potent and selective allosteric BCR-ABL1 inhibitor | €120.00 | |
| 2005 | ASP 3026 | Inhibitor of the oncogenic fusion kinase EML4-ALK | €80.00 | |
| 2219 | AT 9283 | Multitargeted kinase inhibitor (Aurora A/B, JAK2/3, and BCR-Abl) | €85.00 | |
| 2978 | Brigatinib | Potent, selective, and orally active anaplastic lymphoma kinase (ALK) inhibitor | €80.00 | |
| 1660 | Crizotinib | c-MET Inhibitor; NPM-ALK inhibitor | €70.00 | |
| 1392 | Dasatinib | Bcr-Abl and Src tyrosine kinase inhibitor | €90.00 | |
| 2123 | DCC 2036 | An orally active Bcr-ABL inhibitor | €110.00 | |
| 1882 | GNF 2 | Inhibitor of Bcr-Abl tyrosine kinase | €110.00 | |
| 1394 | Imatinib mesylate | Bcr-Abl, c-KIT and PDGFR kinase inhibitor | €60.00 | |
| 2121 | INNO 406 | Dual Bcr-Abl and Lyn kinase inhibitor | €85.00 | |
| 2294 | KRCA 0008 | Potent and selective dual ALK/ACK1 inhibitor with good drug-like properties | €95.00 | |
| 1396 | Nilotinib | BCR-ABL inhibitor | €50.00 | |
| 3168 | Nilotinib hydrochloride | BCR-ABL inhibitor | €70.00 | |
| 1416 | NVP-TAE684 | NPM-ALK inhibitor | €50.00 | |
| 1137 | PD180970 | Bcr-Abl tyrosine kinase inhibitor (p210 specific) | €120.00 | |
| 2600 | PF 06463922 | Potent, orally available and brain-penetrant ALK/ROS1 selective inhibitor | €105.00 | |
| 1407 | SKI 606 | Bcr-Abl and Src tyrosine kinase inhibitor | €75.00 | |