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Dasatinib

Chemical Structure : Dasatinib

CAS No.: 302962-49-8

Dasatinib (BMS-354825, BMS354825)

Catalog No.: PC-42426Not For Human Use, Lab Use Only.

Dasatinib (BMS-354825) is a potent, orally bioavailable, dual Src/Abl kinase inhibitor with IC50 of 0.5, 0.4, 0.5 and <1 nM for Src, Lck, Yes and Bcr-Abl, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Dasatinib (BMS-354825) is a potent, orally bioavailable, dual Src/Abl kinase inhibitor with IC50 of 0.5, 0.4, 0.5 and <1 nM for Src, Lck, Yes and Bcr-Abl, respectively.
Dasatinib (BMS-354825) exhibits two-log increased potency relative to imatinib and retains activity against 14 of 15 imatinib-resistant BCR-ABL mutants.
Dasatinib (BMS-354825) prolongs survival of mice with BCR-ABL-driven disease and inhibits proliferation of BCR-ABL-positive bone marrow progenitor cells from patients with imatinib-sensitive and imatinib-resistant CML.

Physicochemical Properties

M.Wt 488.0056
Formula C22H26ClN7O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: 35.35 mg/mL

Chemical Name/SMILES

5-Thiazolecarboxamide, N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-

References

1. Shah NP, et al. Science. 2004 Jul 16;305(5682):399-401.

2. Schittenhelm MM, et al. Cancer Res. 2006 Jan 1;66(1):473-81.

3. Johnson FM, et al. Clin Cancer Res. 2005 Oct 1;11(19 Pt 1):6924-32.

4. Lombardo LJ, et al. J Med Chem. 2004 Dec 30;47(27):6658-61.

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