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SGI-7079

Cat. No. M2180
SGI-7079 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 60  USD60 In stock
5mg USD 90  USD90 In stock
10mg USD 145  USD145 In stock
50mg USD 565  USD565 In stock
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Quality Control
Biological Activity

SGI-7079 is a novel Axl inhibitor. SGI-7079 decreased IBC cell proliferation, migration and invasion in vitro and inhibited tumor growth of IBC cells in vivo. Mesenchymal cells also expressed increased levels of the receptor tyrosine kinase Axl and showed a trend toward greater sensitivity to the Axl inhibitor SGI-7079, whereas the combination of SGI-7079 with erlotinib reversed erlotinib resistance in mesenchymal lines expressing Axl and in a xenograft model of mesenchymal NSCLC.

Customer Product Validations & Biological Datas
Source Cancer Res (2013). Figure 6. SGI-7079
Method MTT
Cell Lines SUM149 cells
Concentrations 1 mmol/L
Incubation Time 72 h
Results SGI-7079 treatment inhibited the phosphorylation of Axl at Tyr 702 upon Gas6 stimulation in SUM149 cells
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 455.53
Formula C26H26FN7
CAS Number 1239875-86-5
Purity >99%
Solubility DMSO 60 mg/mL
Storage at -20°C
References

[1] Wang X, et al. Cancer Res. TIG1 Promotes the Development and Progression of Inflammatory Breast Cancer through Activation of Axl Kinase.

[2] Byers LA, et al. Clin Cancer Res. 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.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: SGI-7079 supplier, Axl, inhibitors

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