A dual inhibitor of c-Src and Abl
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Saracatinib

Item No. 11497

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methyl-1-piperazinyl)ethoxy]-5-[(tetrahydro-2H-pyran-4-yl)oxy]-4-quinazolinamine
CAS Number
379231-04-6
Synonyms
  • AZD 0530
Molecular Formula
C27H32ClN5O5
Formula Weight
542.0
Purity
≥90%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 0.1 mg/ml
λmax
236, 259 nm
SMILES
ClC1=CC=C2C(OCO2)=C1NC3=NC=NC4=C3C(OC5CCOCC5)=CC(OCCN6CCN(C)CC6)=C4
InChi Code
InChI=1S/C27H32ClN5O5/c1-32-6-8-33(9-7-32)10-13-35-19-14-21-24(23(15-19)38-18-4-11-34-12-5-18)27(30-16-29-21)31-25-20(28)2-3-22-26(25)37-17-36-22/h2-3,14-16,18H,4-13,17H2,1H3,(H,29,30,31)
InChi Key
OUKYUETWWIPKQR-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $35

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    10 mg

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    25 mg

    $119

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    50 mg

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    Product Description

    Saracatinib is a dual inhibitor of the tyrosine kinases c-Src and Abl (IC50 = 2.7 and 30 nM, respectively).1 It less effectively inhibits other receptor and non-receptor tyrosine kinases as well as assorted serine/threonine kinases.1,2,3 Saracatinib is orally available and blocks cell motility, migration, adhesion, invasion, proliferation, differentiation, and survival.1,2,4 Through its effects on c-Src, it reduces osteoclast bone resorption.2 Saracatinib also blocks denque virus RNA replication through its effect on Fyn kinase.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hennequin, L.F., Allen, J., Breed, J., et al. N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-(tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor. J. Med. Chem. 49(22), 6465-6488 (2006).

    2. Allen, J.G., Fotsch, C., and Babij, P. Emerging targets in osteoporosis disease modification. J. Med. Chem. 53(11), 4332-4353 (2010).

    3. Lee, K., Kim, J., Jeong, K.W., et al. Structure-based virtual screening of Src kinase inhibitors. Bioorg. Med. Chem. 17(8), 3152-3161 (2009).

    4. Saad, F., and Lipton, A. SRC kinase inhibition: Targeting bone metastases and tumor growth in prostate and breast cancer. Cancer Treat. Rev. 36(2), 177-184 (2010).

    5. de Wispelaere, M., LaCroix, A.J., and Yang, P.L. The small molecules AZD0530 and dasatinib inhibit dengue virus RNA replication via fyn kinase. J. Virol. 87(13), 7367-7381 (2013).