Dasatinib Inhibitor CAS No. 302962-49-8

Cat. No.	Name	Size	Price	Add Cart
KI0352	Dasatinib	25 mg	$270
KI0352	Dasatinib	100 mg	$662

Chemical Characteristic

Product Name	Dasatinib
Synonyms	SPRYCEL, BMS-354825
CAS No.	302962-49-8
Molecular Weight	488.01
Formula	C₂₂H₂₆ClN₇O₂S
Chemical Name	N-(2-chloro-6-methylphenyl)-2-(6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-ylamino)thiazole-5-carboxamide
Smiles	s1c(ncc1C(=O)Nc1c(cccc1C)Cl)Nc1nc(nc(c1)N1CCN(CC1)CCO)C
Chemical Structure

Biological activities

Dasatinib is a potent dual Src/Abl inhibitor. Dasatinib blocks the kinase activity of imatinib-resistant BCR-ABL mutants where the mutations reside in the activation loop and other sites in the COOH-terminal lobe. ^[1] The IC50 values of dasatinib against wild type Abl, Src and Lyn are 0.6, 0.8 and 2.8 nM, respectively. Dasatinib potently inhibits wild-type Abl kinase and all mutants except T315I over a narrow range (IC50 ??1.7 nM). Dasatinib directly targets wild-type and mutant Abl kinase domains and inhibits autophosphorylation and substrate phosphorylation in a concentration-dependent manner. Dasatinib is an effective single agent therapeutic for cells expressing wild-type Bcr-Abl and all mutants tested except T315I at a trough level of 50 nM. ^[2] Dasatinib potently inhibits WT KIT and juxtamembrane domain mutant KIT autophosphorylation and KIT-dependent activation of downstream pathways important for cell viability and cell survival, such as Ras/mitogen-activated protein kinase, phosphoinositide 3-kinase/Akt, and Janus-activated kinase/signal transducers and activators of transcription. ^[3] Dasatinib inhibits Btk (Bruton's tyrosine kinase) with an IC50 of 5 nM.^[4] Dasatinib at a dose of 10 nM induces a 33% reduction in total cells at 72 hours, increasing to 60% with 150 nM. ^[5] Dasatinib also has activity against cultured human prostate and breast cancer cells. ^[6] Dasatinib specifically inhibits colony formation by LMP2A expressing bone marrow B cells and decreases spleen size in the TgE mice. Spleen mass is markedly reducedd among Dasatinib treated Tg6/λ-MYC mice when compared to the control group. In LMP2A/MYC double transgenic mice, dasatinib prevents lymphadenopathy.^[7] The plasma concentration of dasatinib required to inhibit 90% of phospho-BCR-ABL in vivo is 10.9 ng/mL in mice.^[8]

Protocols

Dasatinib is dissolved in DMSO as a stock solution. ^[4]

References

[1] Tokarski JS, et al. The structure of Dasatinib (BMS-354825) bound to activated ABL kinase domain elucidates its inhibitory activity against imatinib-resistant ABL mutants. Cancer Res. 2006, 66(11): 5790-5797. [2] O'Hare T, et al. In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants. Cancer Res. 2005, 65(11): 4500-4505. [3] Schittenhelm MM, et al. Dasatinib (BMS-354825), a dual SRC/ABL kinase inhibitor, inhibits the kinase activity of wild-type, juxtamembrane, and activation loop mutant KIT isoforms associated with human malignancies. Cancer Res. 2006, 66(1): 473-481. [4] Hantschel O, et al. The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. Proc Natl Acad Sci. 2007, 104(33): 13283-13288. [5] Copland M, et al. Dasatinib (BMS-354825) targets an earlier progenitor population than imatinib in primary CML but does not eliminate the quiescent fraction. Blood. 2006, 107(11): 4532-4539. [6] Nam S, et al. Action of the Src family kinase inhibitor, dasatinib (BMS-354825), on human prostate cancer cells. Cancer Res. 200, 65(20): 9185-9189. [7] Dargart JL, et al. Dasatinib therapy results in decreased B cell proliferation, splenomegaly, and tumor growth in a murine model of lymphoma expressing Myc and Epstein-Barr virus LMP2A. Antiviral Res. 2012, 95(1): 49-56. [8] Luo FR, et al. Dasatinib (BMS-354825) pharmacokinetics and pharmacodynamic biomarkers in animal models predict optimal clinical exposure. Clin Cancer Res. 2006, 12(23): 7180-7186.

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