Y15
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Cat.No：IY0080 Solarbio
CAS：4506-66-5
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to yellow Solid
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> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Angiogenesis > Y15
Product Information
| CAS | 4506-66-5 |
| Name | Y15 |
| Molecular Formula | C6H10N4·4HCl |
| Molecular Weight | 284.01 |
| Solubility | Soluble in Water |
| Purity | ≥98% |
| Appearance | White to yellow Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 224-822-6 |
| MDL | MFCD00012970 |
| SMILES | [H]Cl.[H]Cl.[H]Cl.[H]Cl.NC1=CC(N)=C(N)C=C1N |
| Target Point | FAK |
| Passage | Angiogenesis; Protein Tyrosine Kinase/RTK |
| Background | Y15 specifically inhibits FAK autophosphorylation. |
| Biological Activity | Y15 特异性抑制 FAK 自磷酸化。[1-3] |
| In Vitro | Y15在Panc-1细胞中以0.1μM开始抑制FAK的Y397磷酸化。在100μM的剂量下，Y15具有与TAE226相同或更好的抑制。值得注意的是，在较高剂量的Y15时，总FAK下调。 Y15还阻断FAK下游底物桩蛋白的磷酸化。与FAK类似的较高剂量的总桩蛋白减少。因此，Y15以剂量依赖的方式抑制FAK磷酸化[1]。在所有细胞系(分别为TT，K1，BCPAP和TPC1)上使用一系列Y15剂量完成MTS测定.Y15在所评估的所有甲状腺细胞系中以剂量依赖性方式抑制细胞活力。 TT，TPC1，BCPAP和K1的IC50分别为2.05，5.74，9.99和17.54μM[2]。 |
| In Vivo | 携带Panc si-ctrl异种移植物的裸鼠用TAE226(双FAK和IGF-1R酪氨酸激酶抑制剂)处理，以提供FAK和IGF-1R双重抑制的抗肿瘤作用的参考。在没有药物治疗的情况下，Panc si5-IGF-1R异种移植物比Panc si-ctrl异种移植物(Panc si5-IGF-1R/PBS与Panc si-ctrl/PBS)生长缓慢，表明通过仅抑制IGF-1R途径来抑制中度肿瘤。通过Y15处理进一步抑制FAK活性更显著地抑制Panc si5-IGF-1R异种移植物的生长(Panc si5-IGF-1R/PBS对Panc si5-IGF-1R/Y15)。在用TAE226处理的Panc si-ctrl异种移植物中观察到类似的抗肿瘤作用(Panc si5-IGF-1R/Y15对比Panc si-ctrl/TAE226)。在整个实验过程中，小鼠表现出正常的梳理和饮食习惯[3]。 |
| Cell Experiment | 用不同浓度的Y15或TAE226处理细胞24小时。加入来自Promega Viability试剂盒的3-(4，5-二甲基噻唑-2-基)-5-(3-羧基甲氧基苯基)-2-(4-磺基苯基)-2H-四唑鎓化合物，并将细胞在37°温育。 C持续1-2小时。用酶标仪在490nm处分析96-板上的光密度以确定细胞活力。此外，用Y15处理24小时后用台盼蓝染色细胞，用血细胞计数器测定染色阳性的细胞百分比[1] |
| Animal Experiment | 小鼠[3]使用6周龄的雌性裸鼠。将5×10 6个Panc si5-IGF-1R细胞与基质胶混合并皮下注射到无胸腺裸鼠的侧腹(第0天)。在第7天将动物随机分成两组。一组(n = 5)接受Y15(30mg/kg)，另一组接受PBS作为对照处理(n = 5)。对于Panc si-ctrl异种移植物，将5×106 Panc si-ctrl细胞与基质胶混合并皮下注射到裸鼠的侧腹。这些动物在第7天也随机分成两组，一组(n = 5)接受TAE226(30mg/kg)，另一组接受PBS(n = 5)作为对照处理。通过腹膜内注射施用药物和PBS，总体积为0.1mL。从第10天开始每3或4天测量肿瘤大小的长度(mm)×宽度(mm)。肿瘤体积计算为体积(cm 3)= 1/2×长度(cm)×宽度(cm)2。 |
| Kinase Experiment | 在激酶缓冲液中的10μCi[γ-32P] -ATP将20mM HEPES，pH7.4，5mM MgCl 2，5mM MnCl 2，0.1mM Na 3 VO 4与0.1μg纯化的FAK蛋白在含有10μCi[10μCi]的激酶缓冲液中温育。 γ-32P] -ATP。激酶反应在室温下进行5分钟，并通过加入2×Laemmli缓冲液终止。在Ready SDS-10％PAGE凝胶上分离蛋白质，通过放射自显影观察磷酸化的烯醇化酶[1] |
| Data Literature Source | [1]. Hochwald SN，et al. A novel small molecule inhibitor of FAK decreases growth of human pancreatic cancer. Cell Cycle. 2009 Aug;8(15):2435-43. [2]. O'Brien S，et al. FAK inhibition with small molecule inhibitor Y15 decreases viability，clonogenicity，and cell attachment in thyroid cancer cell lines and synergizes with targeted therapeutics. Oncotarget. 2014 Sep 15;5(17):7945-59. [3]. Zheng D，et al. A novel strategy to inhibit FAK and IGF-1R decreases growth of pancreatic cancer xenografts. Mol Carcinog. 2010 Feb;49(2):200-9. |
| Unit | Bottle |
| Specification | 10mg 10mM*1mL in DMSO 25mg 50mg |
Y15 特异性抑制 FAK 自磷酸化。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
Note：
1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
2. For your safety and health, please wear laboratory clothes, disposable gloves and masks.
3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
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