Kinases (Tyrosine Specific 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.

 

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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) €90.00
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
1392 Dasatinib Bcr-Abl and Src tyrosine kinase inhibitor €95.00
2123 DCC 2036 An orally active Bcr-ABL inhibitor €125.00
1882 GNF 2 Inhibitor of Bcr-Abl tyrosine kinase €125.00
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 €75.00
1416 NVP-TAE684 NPM-ALK inhibitor €70.00
1137 PD 180970 Bcr-Abl tyrosine kinase inhibitor (p210 specific) €120.00
1660 PF 02341066 c-MET Inhibitor; NPM-ALK inhibitor €80.00
2600 PF 06463922 Potent, orally available and brain-penetrant ALK/ROS1 selective inhibitor €105.00

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