{{cart_num}}
My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > MAPK > AZD-8330CAS：869357-68-6
Molecular Formula：C16H17FIN3O4
Molecular Weight：461.23
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Solid
Qty：
Size：
| CAS | 869357-68-6 |
| Name | AZD-8330 |
| Molecular Formula | C16H17FIN3O4 |
| Molecular Weight | 461.23 |
| Solubility | Soluble in DMSO ≥10mg/mL |
| Purity | ≥98% |
| Appearance | Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 642-441-7 |
| MDL | MFCD18384989 |
| SMILES | CC1=CC(=C(N(C1=O)C)NC2=C(C=C(C=C2)I)F)C(=O)NOCCO |
| Target Point | MEK |
| Passage | MAPK |
| Background | AZD8330 is a potent and non-competitive MEK1/MEK2 inhibitor. |
| Biological Activity | AZD8330 是一种有效的非竞争性的 MEK1/MEK2 抑制剂，IC50 为 7 nM。[1-2] |
| IC50 | MEK1:7nM;mEK2:7nM [1-2] |
| In Vitro | AZD8330是一种选择性变构MEK1 / MEK2抑制剂。将人骨肉瘤细胞系MOS，U2OS和143B暴露于浓度为0.5μM的Trametinib，AZD8330或TAK-733 6小时，导致ERK磷酸化丧失，表明有效的MEK抑制。使用浓度测试这三种抑制剂的活性。六种骨肉瘤细胞系中的范围：MOS，U2OS，KPD，ZK58，143b和Saos-2。所有三种抑制剂都降低了MOS和U2OS的活力，并且强烈影响143b。相比之下，KPD，ZK58和Saos-2的活力不受任何三种抑制剂的影响[2]。 |
| In Vivo | 在肿瘤异种移植模型中，AZD8330在耐受剂量(1.0 mg / kg每日一次[OD])下显示出约90％的剂量依赖性肿瘤生长抑制[1]。 |
| Cell Experiment | 人骨肉瘤细胞系MOS，U2OS，143B，ZK58，KPD和Saos-2在补充有10％胎牛血清和25U / mL青霉素和25μg/ mL青霉素 - 链霉素的RPMI1640培养基中生长。将所有细胞在37℃，5％CO 2的潮湿培养箱中培养。如图所示，Trametinib，AZD8330(10nM，100nM和1μM)和TAK-733在6个骨肉瘤细胞系中的剂量响应曲线。将细胞暴露72小时。使用ATPlite 1Step试剂盒处理细胞，然后在读板器上进行发光测量[2]。 |
| Data Literature Source | [1]. Cohen RB，et al. A phase I dose-finding，safety and tolerability study of AZD8330 in patients with advanced malignancies. Eur J Cancer. 2013 May;49(7):1521-9. [2]. Baranski Z，et al. MEK inhibition induces apoptosis in osteosarcoma cells with constitutive ERK1/2 phosphorylation. Genes Cancer. 2015 Nov;6(11-12):503-12. |
| Unit | Bottle |
| Specification | 1mg 5mg |
AZD8330 是一种有效的非竞争性的 MEK1/MEK2 抑制剂。
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.
Sorry, there is no more information.
Sorry, there is no more information.
Sorry, there is no more information.
Manual Download
