Home Protein Tyrosine Kinase Axl inhibitor SGI-7079

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SGI-7079 Axl inhibitor

Cat.No.S7847

SGI-7079, a novel selective Axl inhibitor with an IC50 of 58 nM in vitro, inhibits tumor growth in a dose dependent manner and is a potential therapeutic target for overcoming EGFR inhibitor resistance.
SGI-7079 Axl inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 455.53

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Quality Control

Batch: S784701 DMSO]91 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.68%
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99.68

Solubility

In vitro
Batch:

DMSO : 91 mg/mL (199.76 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 455.53 Formula

C26H26FN7

 Storage (From the date of receipt)
CAS No. 1239875-86-5 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=CNC2=NC(=NC(=C12)C3=CC=CC(=C3)CC#N)NC4=CC(=C(C=C4)N5CCN(CC5)C)F

Mechanism of Action

Targets/IC50/Ki
Met
Mer
YES
RET
FLT3
Axl
(Cell-free assay)
58 nM
In vitro
SGI-7079 exhibits a Ki = 5.7 nM for AXL and inhibits Gas6 ligand-induced tyrosine phosphorylation of human AXL expressed in HEK293T cells (EC50 = 100 nM). It inhibits TAM family members MER and Tyro3 similarly as AXL, and shows potent, low nM inhibition of Syk, Flt1, Flt3, Jak2, TrkA, TrkB, PDGFRβ and Ret kinases. Mesenchymal cells express increased levels of the receptor tyrosine kinase Axl and show a trend toward greater sensitivity to this compound.
In vivo
SGI-7079 inhibits tumor growth in a dose-dependent manner, and at the maximum dose, this compound inhibits tumor growth by 67%, compared with control. the combination of this chemical with erlotinib reverses erlotinib resistance in mesenchymal lines expressing Axl and in a xenograft model of mesenchymal NSCLC.
References

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