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SGI-7079 Sale

(Synonyms: 3-[2-[[3-氟-4-(4-甲基-1-哌嗪基)苯基]氨基]-5-甲基-7H-吡咯并[2,3-D]嘧啶-4-基]苯乙腈) 目录号 : GC19330

An Axl kinase inhibitor

SGI-7079 Chemical Structure

Cas No.:1239875-86-5

规格 价格 库存 购买数量
2mg
¥441.00
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5mg
¥651.00
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10mg
¥1,029.00
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50mg
¥3,759.00
现货
100mg
¥4,914.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

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 uM, 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]

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 Properties

Cas No. 1239875-86-5 SDF
别名 3-[2-[[3-氟-4-(4-甲基-1-哌嗪基)苯基]氨基]-5-甲基-7H-吡咯并[2,3-D]嘧啶-4-基]苯乙腈
Canonical SMILES N#CCC1=CC=CC(C2=C3C(NC=C3C)=NC(NC4=CC=C(N5CCN(C)CC5)C(F)=C4)=N2)=C1
分子式 C26H26FN7 分子量 455.53
溶解度 DMSO : ≥ 34 mg/mL (74.64 mM) 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.1952 mL 10.9762 mL 21.9525 mL
5 mM 0.439 mL 2.1952 mL 4.3905 mL
10 mM 0.2195 mL 1.0976 mL 2.1952 mL
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