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| 25mg |
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Purity: ≥98%
SGI-7079 (SGI7079) is a novel, potent and selective Axl inhibitor with potential anti-inflammatory and anticancer activities. It has an IC50 of 0.43 μM for SUM149 and 0.16 μM for KPL-4 cells, which is a significant inhibition of their proliferation. The most deadly type of breast cancer is called inflammatory breast cancer (IBC), however it is unclear what causes this type of cancer to behave aggressively. In vitro, the Axl inhibitor SGI-7079 treatment of IBC cells reduced their malignant characteristics. Lastly, in primary human IBC specimens, TIG1 expression positively correlated with Axl expression. Our findings clarify the malignant properties of IBC and rationalize TIG1 and Axl as promising therapeutic targets in the treatment of IBC. They also show that TIG1 positively modifies the malignant properties of IBC by supporting Axl function.
| Targets |
Met; Mer; YES; RET; FLT3
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|---|---|
| ln Vitro |
SGI-7079 has an AXL Ki of 5.7 nM and prevents human AXL expressed in HEK293T cells from being tyrosine phosphorylated by Gas6 ligand (EC50 = 100 nM). As with AXL, it inhibits MER and Tyro3, members of the TAM family, and it inhibits Syk, Flt1, Flt3, Jak2, TrkA, TrkB, PDGFRβ, and Ret kinases with strong, low nM activity. The receptor tyrosine kinase Axl is expressed at higher levels in mesenchymal cells, and they also exhibit a tendency to be more sensitive to the Axl inhibitor SGI-7079[2].
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| ln Vivo |
SGI-7079 reduces the growth of tumors in a dose-dependent manner; at the highest dose, the reduction in tumor growth is 67% when compared to the control. In xenograft models of mesenchymal NSCLC and mesenchymal lines expressing Axl, the combination of SGI-7079 and erlotinib reverses erlotinib resistance[2].
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| Cell Assay |
In order to demonstrate the inhibition of Axl activation by SGI-7079, 1 mg of the FLAG-tagged plasmid containing the human Axl gene is electroporated into HEK-293 cells, causing them to transiently transfect. The cells are then incubated for 24 hours in standard media plus 10% FBS. SGI-7079 is applied to cells at the specified concentrations for ten minutes. Gas6-containing WI38 conditioned media is used to stimulate the cells five minutes prior to lysis.
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| Animal Protocol |
Mouse(NCr-nu/nu female mice) xenograft model of NSCLC using the mesenchymal NSCLC cell line A549
10, 25, 50 mg/kg p.o. |
| References |
| Molecular Formula |
C26H26FN7
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|---|---|
| Molecular Weight |
455.5299
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| Exact Mass |
455.223
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| Elemental Analysis |
C, 68.55; H, 5.75; F, 4.17; N, 21.52
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| CAS # |
1239875-86-5
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| Related CAS # |
1239875-86-5
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| PubChem CID |
46870258
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.675
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| LogP |
3.24
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
34
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| Complexity |
719
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1C([H])=C(C([H])=C([H])C=1N1C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])C1([H])[H])N([H])C1N=C2C(C(C([H])([H])[H])=C([H])N2[H])=C(C2=C([H])C([H])=C([H])C(C([H])([H])C#N)=C2[H])N=1
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| InChi Key |
BCFKACXAIBEPKR-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
2-[3-[2-[3-fluoro-4-(4-methylpiperazin-1-yl)anilino]-5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]phenyl]acetonitrile
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| Synonyms |
SGI7079; SGI 7079; SGI-7079
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~91 mg/mL (~199.8 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.17 mg/mL (4.76 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.17 mg/mL (4.76 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1952 mL | 10.9762 mL | 21.9525 mL | |
| 5 mM | 0.4390 mL | 2.1952 mL | 4.3905 mL | |
| 10 mM | 0.2195 mL | 1.0976 mL | 2.1952 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 Axl inhibitor SGI-7079 inhibited the proliferation, migration, and invasion of IBC cells.Cancer Res.2013 Nov 1;73(21):6516-25. |
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 Mesenchymal lines are significantly more resistant to EGFR inhibition and PI3K pathway inhibition but sensitive to Axl inhibition by SGI-7079.Clin Cancer Res.2013 Jan 1;19(1):279-90. |
 Axl blockade by SGI-7079 inhibits the growth of mesenchymal NSCLC xenograft tumors.(A) Mean tumor volume for A549 xenografts implanted in mice treated with vehicle or SGI-7079. (B) Mean tumor volume for A549 xenografts in mice treated with vehicle and the combination of SGI-7079 plus erlotinib.Clin Cancer Res.2013 Jan 1;19(1):279-90. |
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