An Axl kinase inhibitor
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SGI-7079

Item No. 20111

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[2-[[3-fluoro-4-(4-methyl-1-piperazinyl)phenyl]amino]-5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-benzeneacetonitrile
CAS Number
1239875-86-5
Molecular Formula
C26H26FN7
Formula Weight
455.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml
λmax
285 nm
SMILES
CN1CCN(C2=C(F)C=C(NC3=NC(C4=CC(CC#N)=CC=C4)=C(C(C)=CN5)C5=N3)C=C2)CC1
InChi Code
InChI=1S/C26H26FN7/c1-17-16-29-25-23(17)24(19-5-3-4-18(14-19)8-9-28)31-26(32-25)30-20-6-7-22(21(27)15-20)34-12-10-33(2)11-13-34/h3-7,14-16H,8,10-13H2,1-2H3,(H2,29,30,31,32)
InChi Key
BCFKACXAIBEPKR-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $145

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    10 mg

    $268

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    25 mg

    $502

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    Product Description

    SGI-7079 is an inhibitor of the receptor tyrosine kinase Axl.1 It inhibits proliferation of inflammatory breast cancer cells (IC50s = 0.43 and 0.15 µM for SUM149 and KPL-4 cells, respectively), decreases invasion, and halts the cell cycle in the G1 phase. SGI-7079 synergistically increases the potency of erlotinib (Item No. 10483) on EGFR inhibition.2 In a mouse xenograft model of non-small cell lung cancer, SGI-7079 dose-dependently inhibits tumor growth, an effect that is greater when used in combination with erlotinib.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wang, X., Saso, H., Iwamoto, T., et al. TIG1 promotes the development and progression of inflammatory breast cancer through activation of Axl kinase. Cancer Res. 73(21), 6516-6525 (2013).

    2. Byers, L.A., Diao, L., Wang, J., et al. An epithelial-mesenchymal transition gene signature predicts resistance to EGFR and PI3K inhibitors and identifies Axl as a therapeutic target for overcoming EGFR inhibitor resistance. Clin. Cancer Res. 19(1), 279-290 (2013).