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AG 1296,≥98% (HPLC)

别名:AG-1296;AG1296;6,7-Dimethoxy-3-phenylquinoxaline;6,7-二甲氧基-2-苯基喹喔啉

CAS号 146535-11-7 经验分子式(希尔表示法) C16H14N2O2 分子量 266.29 MDL number MFCD00270913
货号(SKU): 658551
CAS号: 146535-11-7
MDL号: MFCD00270913
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$362.97

产品描述

一种有效的和选择性的PDGFR抑制剂,IC500:0.4μm。也抑制Bek(FGF受体)酪氨酸激酶和c-kit。

General description

Similar to but more potent than AG 1295 (Cat. No. 658550). A cell-permeable, reversible, and ATP-competitive, inhibitor of PDGF receptor kinase and blocks signaling of human PDGF α-receptors (IC50 = 1.0 µM) and β-receptors (IC50 = 800 nM) as well as of the related stem cell factor receptor c-kit (80% inhibition at 5 µM). Affects neither the binding of PDGF-BB to the PDGF-β receptor nor the receptor dimerization. Has no effect on autophosphorylation of the vascular endothelial growth factor receptor KDR or on DNA synthesis induced by vascular endothelial growth factor in porcine aortic endothelial cells. Also reverses the transformed phenotype of sis-transfected NIH/3T3 cells but has no effect on src-transformed NIH 3T3 cells or on the activity of the kinase p60c-src (F257) immunoprecipitated from these cells. Potently inhibits autophosphorylation in Flt3/Tel-BaF3 and Flt3/Itd-BaF3 cells with an IC50 of 300 nM and ~1 µM, respectively.

包装

5 mg in Plastic ampoule

Biochem/physiol Actions

Cell permeable: yes

Primary Target
PDGFR kinase

Product competes with ATP.

Reversible: yes

Target IC50: 1.0 µM, 800 nM, against signaling of human PDGF α-receptors, human PDGF β-receptors, respectively

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Other Notes

Tse, KF., et al. 2002. Leukemia16, 2027.
Tse, KF., et al. 2001. Leukemia15, 1001.
Strutz, F., et al. 2001. Kidney Int.59, 579.
Kovalenko, M., et al. 1997. Biochemistry 36, 6260.
Kovalenko, M., et al. 1994. Cancer Res. 54, 6106.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

性质

Quality Level  100
assay  ≥98% (HPLC)
form  solid
mfr. no.  Calbiochem®
storage condition  OK to freeze
 protect from light
storage conditions  -20C
color  white
solubility  DMSO: 10 mg/mL
 acetonitrile: soluble
shipped in  ambient
InChI  1S/C16H14N2O2/c1-19-15-8-12-13(9-16(15)20-2)18-14(10-17-12)11-6-4-3-5-7-11/h3-10H,1-2H3
InChI key  QNOXYUNHIGOWNY-UHFFFAOYSA-N


安全信息

WGK德国 WGK 3
商品规格
属性名称属性值
储存温度 Storage temp.-20°C低温冷冻
全球实时库存 Availability √美国St. Louis ≥ 55 | 欧洲Eur. ≥ 16 | 東京Tokyo ≥ 8 | 香港与北京 ≥ 10