CAS 1239875-86-5|SGI-7079

Introduction：Basic information about CAS 1239875-86-5|SGI-7079, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. SGI-7079 BiologicalActivity
3. Chemical & Physical Properties
4. Synonyms

Common Name	SGI-7079
CAS Number	1239875-86-5	Molecular Weight	455.530
Density	1.3±0.1 g/cm3	Boiling Point	/
Molecular Formula	C₂₆H₂₆FN₇	Melting Point	/
MSDS	/	Flash Point	/

Names

Name	2-(3-(2-(3-Fluoro-4-(4-methylpiperazin-1-yl)phenylamino)-5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl)acetonitrile
Synonym	More Synonyms

SGI-7079 BiologicalActivity

Description	SGI-7079 is an Axl inhibitor, significantly inhibits the proliferation of SUM149 or KPL-4 cells with an IC50 of 0.43 or 0.16 μM, respectively.Ic50 value:Target: Axlin vitro: SGI-7079 treatment inhibits the phosphorylation of Axl at Tyr 702 upon Gas6 stimulation in SUM149 cells. The growth of SUM149 and KPL-4 in soft agar, one of the hallmark characteristics of cellular transformation and uncontrolled cell growth, is also significantly inhibited by SGI-7079 treatment. SGI-7079 treatment also significantly decreases the migration and invasion of SUM149 cells and the invasion of KPL-4 cells. Taken together, Axl inhibitor SGI-7079 significantly inhibits the proliferation, migration, and invasion of IBC cells, suggesting that Axl may be a promising therapeutic target in patients with IBC. [1]in vivo: SGI-7079 inhibits tumor growth in a dose dependent manner, and at the maximum dose, inhibited tumor growth by 67%, compared to control. The combined inhibition of Axl (SGI-7079) plus EGFR (Erlotinib) is significantly more effective than either drug alone. Notably, SGI-7079 + Erlotinib (25/100 mg/kg) reduced the tumor growth by 82%. Axl blockade by SGI-7079 inhibits the growth of mesenchymal NSCLC xenograft tumors. [2]
Related Catalog	Signaling Pathways >>Protein Tyrosine Kinase/RTK >>TAM ReceptorResearch Areas >>Cancer
References	[1]. Wang X, et al. TIG1 promotes the development and progression of inflammatory breast cancer through activation of Axl kinase. Cancer Res. 2013 Nov 1;73(21):6516-25. [2]. Byers LA, 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. 2013 Jan 1;19(1):279-90.

Description

SGI-7079 is an Axl inhibitor, significantly inhibits the proliferation of SUM149 or KPL-4 cells with an IC50 of 0.43 or 0.16 μM, respectively.Ic50 value:Target: Axlin vitro: SGI-7079 treatment inhibits the phosphorylation of Axl at Tyr 702 upon Gas6 stimulation in SUM149 cells. The growth of SUM149 and KPL-4 in soft agar, one of the hallmark characteristics of cellular transformation and uncontrolled cell growth, is also significantly inhibited by SGI-7079 treatment. SGI-7079 treatment also significantly decreases the migration and invasion of SUM149 cells and the invasion of KPL-4 cells. Taken together, Axl inhibitor SGI-7079 significantly inhibits the proliferation, migration, and invasion of IBC cells, suggesting that Axl may be a promising therapeutic target in patients with IBC. [1]in vivo: SGI-7079 inhibits tumor growth in a dose dependent manner, and at the maximum dose, inhibited tumor growth by 67%, compared to control. The combined inhibition of Axl (SGI-7079) plus EGFR (Erlotinib) is significantly more effective than either drug alone. Notably, SGI-7079 + Erlotinib (25/100 mg/kg) reduced the tumor growth by 82%. Axl blockade by SGI-7079 inhibits the growth of mesenchymal NSCLC xenograft tumors. [2]

Related Catalog

Signaling Pathways >>Protein Tyrosine Kinase/RTK >>TAM ReceptorResearch Areas >>Cancer

References

[1]. Wang X, et al. TIG1 promotes the development and progression of inflammatory breast cancer through activation of Axl kinase. Cancer Res. 2013 Nov 1;73(21):6516-25.

[2]. Byers LA, 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. 2013 Jan 1;19(1):279-90.

Chemical & Physical Properties

Density	1.3±0.1 g/cm3
Molecular Formula	C₂₆H₂₆FN₇
Molecular Weight	455.530
Exact Mass	455.223358
PSA	83.87000
LogP	3.24
Index of Refraction	1.675
InChIKey	BCFKACXAIBEPKR-UHFFFAOYSA-N
SMILES	Cc1c[nH]c2nc(Nc3ccc(N4CCN(C)CC4)c(F)c3)nc(-c3cccc(CC#N)c3)c12
Storage condition	-20℃

Synonyms

Benzeneacetonitrile, 3-[2-[[3-fluoro-4-(4-methyl-1-piperazinyl)phenyl]amino]-5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-

sgi-7079

[3-(2-{[3-Fluoro-4-(4-methyl-1-piperazinyl)phenyl]amino}-5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl]acetonitrile

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