Dasatinib (free base)
Catalog #:
IN0127
IN0127-25mg | USD126.0 |
IN0127-100mg | USD270.0 |
Synonyms: Dasatinib, Sprycel, N-(2-CHLORO-6-METHYLPHENYL)-2-({6-[4-(2-HYDROXYETHYL)PIPERAZIN-1-YL]-2-METHYLPYRIMIDIN-4-YL}AMINO)-1,3-THIAZOLE-5-CARBOXAMIDE, BMS-354825
IUPAC Name:
N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)piperazin-1-yl]-2- methylpyrimidin-4-yl]amino]-1,3-thiazole-5-carboxamide
Functional Activity:
Dasatinib is the potent inhibitor of BCR/ABL, Src, c-Kit, multiple Eph kinases, and several other tyrosine kinases, but not erbB kinases such as EGFR or Her2.
It is now a cancer drug for use in patients with chronic myelogenous leukemia (CML) after imatinib treatment and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL). It is being evaluated for use in numerous other cancers, including advanced prostate cancer.
Technical Data:
M.Wt: 488.01
Formula: C22H26 ClN7O2S
Solubility: Soluble in DMSO
Purity: >99%
Storage: Store at -20°C
CAS No.: 302962-49-8
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References for Dasatinib:
1. Yu, E. Y., Wilding, G., Posadas, E., Gross, M., Culine, S., Massard, C., Morris, M. J., Hudes, G., Calabro, F., Cheng, S., Trudel, G. C., Paliwal, P., and Sternberg, C. N. Phase II study of dasatinib in patients with metastatic castration-resistant prostate cancer. Clin Cancer Res, 15: 7421-7428, 2009.
2. Konecny, G. E., Glas, R., Dering, J., Manivong, K., Qi, J., Finn, R. S., Yang, G. R., Hong, K. L., Ginther, C., Winterhoff, B., Gao, G., Brugge, J., and Slamon, D. J. Activity of the multikinase inhibitor dasatinib against ovarian cancer cells. Br J Cancer, 101: 1699-1708, 2009.
3. Ceppi, P., Papotti, M., Monica, V., Lo Iacono, M., Saviozzi, S., Pautasso, M., Novello, S., Mussino, S., Bracco, E., Volante, M., and Scagliotti, G. V. Effects of Src kinase inhibition induced by dasatinib in non-small cell lung cancer cell lines treated with cisplatin. Mol Cancer Ther, 8: 3066-3074, 2009.
4. Araujo, J. C., Poblenz, A., Corn, P., Parikh, N. U., Starbuck, M. W., Thompson, J. T., Lee, F., Logothetis, C. J., and Darnay, B. G. Dasatinib inhibits both osteoclast activation and prostate cancer PC-3-cell-induced osteoclast formation. Cancer Biol Ther, 8: 2153-2159, 2009.
5. Hegedus, C., Ozvegy-Laczka, C., Apati, A., Magocsi, M., Nemet, K., Orfi, L., Keri, G., Katona, M., Takats, Z., Varadi, A., Szakacs, G., and Sarkadi, B. Interaction of nilotinib, dasatinib and bosutinib with ABCB1 and ABCG2: implications for altered anti-cancer effects and pharmacological properties. Br J Pharmacol, 158: 1153-1164, 2009.
6. Koreckij, T., Nguyen, H., Brown, L. G., Yu, E. Y., Vessella, R. L., and Corey, E. Dasatinib inhibits the growth of prostate cancer in bone and provides additional protection from osteolysis. Br J Cancer, 101: 263-268, 2009.