AZD-3463
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Cat.No：IA3650 Solarbio
CAS：1356962-20-3
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Solid
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> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Protein Tyrosine Kinase/PTK > AZD-3463
Product Information
| CAS | 1356962-20-3 |
| Name | AZD-3463 |
| Molecular Formula | C24H25ClN6O |
| Molecular Weight | 448.95 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| SMILES | ClC(C=NC(NC1=C(OC)C=C(N2CCC(N)CC2)C=C1)=N3)=C3C4=CNC5=C4C=CC=C5 |
| Target Point | IGF-1R，ALK |
| Passage | Protein Tyrosine Kinase/RTK;Angiogenesis |
| Background | AZD-3463 is an ALK/IGF1R inhibitor. |
| Biological Activity | AZD3463是一种新型的，有效的 ALK 抑制剂，Ki为0.75 nM，也等效抑制 IGF1R。AZD3463 可通过诱导细胞凋亡和自噬来抑制细胞活力。[1-2] |
| In Vitro | AZD-3463对一些临床相关的Crizotinib耐药突变型具有良好的活性，包括gatekeeper突变型L1196M，在体外作用于含EML4-ALK的Ba/F3细胞系，观察到同等有效作用于野生型ALK。[1]AZD3463有效作用于ALK驱动的临床前期模型和各种耐Crizotinib的模型。AZD3463作用于含ALK融合的肿瘤细胞系，包括DEL(ALCL NPM-ALK)，H3122(NSCLC EML4-ALK)和H2228(NSCLC EML4-ALK)，抑制ALK，降低ALK自身磷酸化。抑制ALK会干扰下游信号包括ERK，AKT和STAT3通路，导致优先抑制含ALK融合的细胞系增殖。为了进一步评估AZD3463克服耐药机制的潜力，评估作用于多个耐Crizotinib的细胞系的抗增殖活性，这些耐Crizotinib的细胞系是从H3122细胞及Crizotinib复发病人衍生的。这些包含多重耐药机制的抗性细胞系包括L1196M gatekeeper和T115Ins突变型。AZD3463在体外作用于这些耐药模型，对12分之10的细胞具有抗增殖的效力，是亲本H3122细胞的4倍。[2] |
| In Vivo | AZD-3463在体内作用于移植瘤，抑制pALK，这种作用存在剂量依赖性，导致肿瘤体积停滞(H3122)或衰退(DEL，H2228)。在体内，AZD-3463同等有效作用于突变型L1196M和野生型ALK。[1]AZD3463在体内作用于移植瘤，抑制pALK，这种作用存在剂量依赖性，导致停滞(H3122)或衰退(DEL，H2228)。[2] |
| Data Literature Source | [1] 104th AACR meeting，2013，Abst 919. [2] Christabel Wilson，et al. Scientific Reports. 2017，7:13955. |
| Unit | Bottle |
| Specification | 5mg 10mg |
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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