Dasatinib - CAS 302962-49-8

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BP-300077 25 g $489 In stock
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Dasatinib, also known as BMS-354825, is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib binds to and inhibits the growth-promoting activities of these kinases. Apparently because of its less stringent binding affinity for the BCR-ABL kinase, dasatinib has been shown to overcome the resistance to imatinib of chronic myeloid leukemia (CML) cells harboring BCR-ABL kinase domain point mutations. SRC-family protein-tyrosine kinases interact with variety of cell-surface receptors and participate in intracellular signal transduction pathways; tumorigenic forms can occur through altered regulation or expression of the endogenous protein and by way of virally-encoded kinase genes.

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Molecular Formula
C22H26ClN7O2S
Molecular Weight
488.01

Dasatinib

    • Specification
      • Related CAS
        854001-07-3 (hydrochloride) 863127-77-9 (Monohydrate)
        Purity
        >98%
        Appearance
        White to Off-White Solid
        Synonyms
        BMS-354825; BMS354825; BMS354825
    • Properties
      • Melting Point
        >250°C (dec.)
        InChI Key
        ZBNZXTGUTAYRHI-UHFFFAOYSA-N
        InChI
        InChI=1S/C22H26ClN7O2S/c1-14-4-3-5-16(23)20(14)28-21(32)17-13-24-22(33-17)27-18-12-19(26-15(2)25-18)30-8-6-29(7-9-30)10-11-31/h3-5,12-13,31H,6-11H2,1-2H3,(H,28,32)(H,24,25,26,27)
        Canonical SMILES
        CC1=C(C(=CC=C1)Cl)NC(=O)C2=CN=C(S2)NC3=NC(=NC(=C3)N4CCN(CC4)CCO)C
    • Reference Reading
      • 1.Successful pregnancy involving a man with chronic myeloid leukemia on dasatinib
        Houssam Oweini • Zaher K. Otrock. Arch Gynecol Obstet (2011) 283:133–134
        On January 2008, dasatinib (70 mg twice daily) was started. The patient tolerated treatment well with no significant side effects. He was being followed up regularly with blood studies. By the end of February 2009 he informed us that his wife had a successful delivery of a healthy baby boy after a full term pregnancy. The baby was 3.1 kg and 46 cm with no congenital anomalies. At the time of conception, the patient was receiving dasatinib 140 mg/day, and the cumulative dose of dasatinib was approximated 350 g. At the time of writing this report, the patient was doing well on dasatinib. His last evaluation showed that he was in complete hematological response with no molecular response (quantitative analysis of peripheral blood BCR-ABL mRNA levels using real-time polymerase chain reaction were 6.00E-2, relative expression ratio of bcr-abl to G6PDH (ROCHE Diagnostics, Light Cycler 2.0). His baby was 7 months old, and he was in good health.
        2.H2-receptor antagonist influences dasatinib pharmacokinetics in a patient with Philadelphia-positive acute lymphoblastic leukemia
        Akihito Matsuoka • Naoto Takahashi • Masatomo Miura • Takenori Niiok. Cancer Chemother Pharmacol (2012) 70:351–352
        Takahashi et al. recently reported in this journal that administration of an acid suppressant such as an H2-receptor antagonist (H2RA) and a proton pump inhibitor can decrease the absorption of dasatinib from the gastrointestinal tract, thereby resulting in a significant decrease in plasma dasatinib concentration. Here, we report a patient treated with dasatinib and H2RA famotidine whose plasma dasatinib concentration increased dramatically after the cessation of famotidine.
    • Preparing Stock Solutions
      • ConcentrationVolumeMass1 mg5 mg10 mg
        1 mM2.0491 mL10.2457 mL20.4914 mL
        5 mM0.4098 mL2.0491 mL4.0983 mL
        10 mM0.2049 mL1.0246 mL2.0491 mL
        50 mM0.0410 mL0.2049 mL0.4098 mL
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Tip: Chemical formula is case sensitive. C22H30N4O c22h30n40
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