A Raf kinase inhibitor
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AZ 628

Item No. 15336

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-(1-cyano-1-methylethyl)-N-[3-[(3,4-dihydro-3-methyl-4-oxo-6-quinazolinyl)amino]-4-methylphenyl]-benzamide
CAS Number
878739-06-1
Molecular Formula
C27H25N5O2
Formula Weight
451.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 0.25 mg/ml
λmax
220, 225, 316 nm
SMILES
CC(C)(C#N)C1=CC=CC(C(NC2=CC(NC3=CC(C(N(C)C=N4)=O)=C4C=C3)=C(C)C=C2)=O)=C1
InChi Code
InChI=1S/C27H25N5O2/c1-17-8-9-21(31-25(33)18-6-5-7-19(12-18)27(2,3)15-28)14-24(17)30-20-10-11-23-22(13-20)26(34)32(4)16-29-23/h5-14,16,30H,1-4H3,(H,31,33)
InChi Key
ZGBGPEDJXCYQPH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $103

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    10 mg

    $186

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    25 mg

    $420

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    Product Description

    AZ 628 is a quinazilinone that inhibits several Raf kinases, including B-Raf, B-RafV600E, and c-Raf-1 (IC50s = 105, 34, and 29 nM in in vitro kinase assays).1,2 It also prevents activation of several tyrosine kinases, including VEGFR2, DDR2, Lyn, Flt1, and FMS.1 In colon and melanoma cell lines carrying B-RafV600E mutations, AZ 628 is reported to inhibit anchorage-dependent and -independent growth, induce cell cycle arrest, and cause apoptosis.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Khazak, V., Astsaturov, I., Serebriiskii, I.G., et al. Selective Raf inhibition in cancer therapy. Expert Opin. Ther. Targets 11(12), 1587-1609 (2007).

    2. Montagut, C., Sharma, S.V., Shioda, T., et al. Elevated CRAF as a potential mechanism of acquired resistance to BRAF inhibition in melanoma. Cancer Res. 68(12), 4853-4861 (2008).