ANI-7  ≥98%

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包装规格:10mg in glass bottle
溶解性:溶于DMSO(20.83 mg/mL 超声)
产品描述:基本信息 产品编号: A11362 产品名称: ANI-7 CAS: 931417-26-4   储存条件 粉末 -20℃ 四年     分子式: C13H8Cl2N2 溶于液体 -80℃ 六个月 分子量 263.12 -20℃ 一个月 化学名:  (Z)-2-(3,4-dichlorophenyl)-3-(1H-pyrrol-2-yl)prop-2-enenitrile Solubility (25°C):   体外:   DMSO 20mg/mL(76.0109mM;Need ultrasonic) Ethanol   Water   体内(现配现用): 1.请依序添加每种溶剂:10% DMSO→40% PEG300→5% Tween-80→45% saline,Solubility:≥2.08mg/mL(7.91mM);Clear solution 此⽅案可获得≥2.08mg/mL(7.91mM,饱和度未知)的澄清溶液。以1mL⼯作液为例,取100μL20.8mg/mL的澄清DMSO储备液加到400μLPEG300中,混合均匀;向上述体系中加⼊50μLTween-80,混合均匀;然后继续加⼊450μL⽣理盐⽔定容⾄1mL。 2.请依序添加每种溶剂:10% DMSO→90% corn oil Solubility:≥2.08mg/mL(7.91mM);Clear solution 此⽅案可获得≥2.08mg/mL(7.91mM,饱和度未知)的澄清溶液,此⽅案不适⽤于实验周期在半个⽉以上的实验。以1mL⼯作液为例,取100μL20.8mg/mL的澄清DMSO储备液加到900μL⽟⽶油中,混合均匀。 <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 3.8005mL 19.0027mL 38.0055mL 5mM 0.7601mL 3.8005mL 7.6011mL 10mM 0.3801mL 1.9003mL 3.8005mL   生物活性 产品描述 一种AhR途径的激活剂。ANI-7抑制多种癌细胞的生长,并有选择地抑制MCF-7乳腺癌细胞的生长,GI50为0.56μM。ANI-7通过激活AhR途径诱导CYP1代谢单加氧酶,并在敏感的乳腺癌细胞系中诱导DNA损伤,检查点激酶(Chk2)激活,S期细胞周期停滞和细胞死亡。 靶点 Aryl Hydrocarbon Receptor Chk2 体外研究 ANI-7 (2.5μM; 24 hours; MCF10A and MDA-MB-468 cells) treatment induces significant S-phase and G2 + M-phase cell cycle arrest within 24 hours of treatment in MDA-MB-468 cells, and negligible effect in normal breast MCF10A cells[1] . ANI-7 (2μM; 12-24 hours; MDA-MB-468 cells) treatment results in a significant increase in the content and phosphorylation of CHK2, and induces a significant increase in H2AXɣ in MDA-MB-468 cells, indicative of DNA double-strand damage[1] . Inhibition of the AhR pathway ameliorates the effects of ANI-7. ANI-7 activates XRE activity and expression of the AhR and CYP1 members Comparisons of the GI50 values show that ANI-7 produces a GI50 value of 0.38μM in MCF-7 cells, whereas values of 3.0-42μM are observed in cell lines from lung, colon, ovary, neuronal, glial, prostate, and pancreas. The only other tumor type that shows appreciable growth inhibition by ANI-7 is the A431 vulva cell line (GI50 of 0.51μM)ANI-7 potently inhibits the growth of T47D, ZR-75-1, MCF-7, SKBR3, and MDA-MB-468 breast cancer cells (GI50 range of 0.16- 0.38μM), moderately inhibits the growth of BT20 and BT474 cells (GI50 range of 1-2μM), and essentially fails to inhibit the growth of MDA-MB-231 and MCF10A cells (GI50 range of 17-26μM). Moreover, ANI-7 maintained its ability to inhibit the growth of drug-resistant cells (MCF-7/VP16: GI50 of 0.21μM) Cell Cycle Analysis[1 Cell Line: MCF10A and MDA-MB-468 cells Concentration: 2.5μM Incubation Time: 24 hours Result: Induced significant S-phase and G2 + M-phase cell cycle arrest in MDA-MB-468 cells, and negligible effect in normal breast MCF10A cells. Western Blot Analysis Cell Line: MDA-MB-468 cells Concentration: 2μM Incubation Time: 12 hours, 24 hours Result: Resulted in a significant increase in the content and phosphorylation of CHK2 (25-fold increase),and induced a significant increase in H2AXɣ (3.5-fold increase).
保存条件:-20℃