Dasatinib

1.8

1.8

280-286 °C

280 - 286 °C

Danger

H301 (92.5%): Toxic if swallowed [Danger Acute toxicity, oral]；H315 (77.5%): Causes skin irritation [Warning Skin corrosion/irritation]；H318 (75%): Causes serious eye damage [Danger Serious eye damage/eye irritation]；H351 (80%): Suspected of causing cancer [Warning Carcinogenicity]；H360 (12.5%): May damage fertility or the unborn child [Danger Reproductive toxicity]；H361 (80%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]；H371 (10%): May cause damage to organs [Warning Specific target organ toxicity, single exposure]；H372 (80%): Causes damage to organs through prolonged or repeated exposure [Danger Specific target organ toxicity, repeated exposure]；H373 (15%): May causes damage to organs through prolonged or repeated exposure [Warning Specific target organ toxicity, repeated exposure]；H410 (80%): Very toxic to aquatic life with long lasting effects [Warning Hazardous to the aquatic environment, long-term hazard]

P203, P260, P264, P264+P265, P270, P273, P280, P301+P316, P302+P352, P305+P354+P338, P308+P316, P317, P318, P319, P321, P330, P332+P317, P362+P364, P391, P405, and P501 (click each P-code to see the statement)

Aggregated GHS information provided per 40 reports by companies from 11 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.；Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown. For more detailed information, please visit ECHA C&L website.

L01XE06

L - Antineoplastic and immunomodulating agents；L01 - Antineoplastic agents；L01E - Protein kinase inhibitors；L01EA - Bcr-abl tyrosine kinase inhibitors；L01EA02 - Dasatinib

QL - Antineoplastic and immunomodulating agents；QL01 - Antineoplastic agents；QL01E - Protein kinase inhibitors；QL01EA - Bcr-abl tyrosine kinase inhibitors；QL01EA02 - Dasatinib

L01EA02

Dasatinib is an orally available small-molecule multikinase inhibitor. During clinical trials, less than 1% of patients treated with dasatinib had QTc prolongation as an adverse reaction, and 1% experienced a QTcF higher than 500 ms. The use of dasatinib is also associated with myelosuppression, bleeding-related events, fluid retention, cardiovascular toxicity, pulmonary arterial hypertension, severe dermatologic reactions, tumor lysis syndrome and hepatotoxicity. It may also cause embryo-fetal toxicity and lead to adverse reactions associated with bone growth and development in pediatric patients.

Dasatinib is a tyrosine kinase inhibitor with several targets. At nanomolar concentrations, it inhibits BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ. In patients with chronic myeloid leukemia (CML), the tyrosine kinase activity of BCR-ABL is deregulated, leading to the growth, proliferation and survival of cancerous hematopoietic cells. Dasatinib binds to the active and inactive conformation of the ABL kinase domain with a higher affinity than imatinib. In chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL) cell lines overexpressing BCR-ABL, dasatinib inhibits cell growth. Also, dasatinib has _in vitro_ activity against leukemic cell lines that are either sensitive or resistant to imatinib. It has been suggested that dasatinib is able to overcome imatinib resistance caused by BCR-ABL kinase domain mutations because it does not require interaction with some of the residues involved in those mutations.