Brigatinib
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Cat.No：IB1190 Solarbio
CAS：1197953-54-0
Storage：Powder:-20℃，2 years
Purity：≥98%
Appearance：White to yellow Solid
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> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Protein Tyrosine Kinase/PTK > Brigatinib
Product Information
| CAS | 1197953-54-0 |
| Name | Brigatinib |
| Molecular Formula | C29H39ClN7O2P |
| Molecular Weight | 584.09 |
| Solubility | Soluble in DMSO ≥0.1mg/mL |
| Purity | ≥98% |
| Appearance | White to yellow Solid |
| Storage | Powder:-20℃，2 years |
| EC | EINECS 1592732-453-0 |
| MDL | MFCD29472221 |
| SMILES | CN1CCN(CC1)C2CCN(CC2)C3=CC(=C(C=C3)NC4=NC=C(C(=N4)NC5=CC=CC=C5P(=O)(C)C)Cl)OC |
| InChIKey | AILRADAXUVEEIR-UHFFFAOYSA-N |
| InChI | InChI=1S/C29H39ClN7O2P/c1-35-15-17-37(18-16-35)21-11-13-36(14-12-21)22-9-10-24(26(19-22)39-2)33-29-31-20-23(30)28(34-29)32-25-7-5-6-8-27(25)40(3,4)38/h5-10,19-21H,11-18H2,1-4H3,(H2,31,32,33,34) |
| PubChem CID | 68165256 |
| Target Point | ALK;EGFR;FLT3;IGF-1R;ROS1 |
| Passage | Angiogenesis; Protein Tyrosine Kinase/RTK |
| Background | It is a potent and selective ALK inhibitor. |
| Biological Activity | Brigatinib 是有效，选择性的 ALK 抑制剂，IC50 值为 0.6 nM。[1-3] |
| IC50 | 0.6nM(ALK)[1] |
| In Vitro | Brigatinib有效抑制ALK的体外激酶活性(IC50，0.6 nM)和测试的所有五种突变体变体，包括G1202R(IC50，0.6-6.6 nM)。 Brigatinib表现出高度的选择性，仅抑制11种额外的天然或突变激酶，IC50 1000nM)。在细胞试验中，brigatinib分别抑制ALK和ROS1，IC50分别为14和18 nM。 Brigatinib以低约11倍的效力(IC50，148-158nM)抑制FLT3和IGF-1R，并抑制FLT3和EGFR的突变体变异，效力低15-35倍(IC50，211-489nM)。 Brigatinib在三种ALK阴性ALCL和NSCLC细胞系中抑制细胞生长，GI50值范围为503至2，387 nM [1]。 Brigatinib抑制ALK活性并消除ALK成瘾神经母细胞瘤细胞系的增殖，IC50为75.27±8.89 nM。 Brigatinib分别以10和4 nM水平抑制ALK-I1171N和ALK-G1269A突变受体[3]。 |
| In Vivo | Brigatinib(10，25或50mg / kg每日一次，po)导致ALK + Karpas-299(ALCL)和H2228(NSCLC)异种移植小鼠模型中肿瘤生长的剂量依赖性抑制。与克唑替尼相比，Brigatinib显著增强携带ALK +脑肿瘤的小鼠的存活[1]。 Brigatinib(10，25，50 mg / kg，po)导致剂量依赖性抗肿瘤活性，在NSCLC小鼠模型中具有肿瘤消退[2]。 |
| Cell Experiment | 以每孔15，000个细胞接种细胞，连续稀释所示抑制剂。 72小时后，通过刃天青评估细胞活力。通过将数据拟合至log(抑制剂浓度)与标准化响应(可变斜率)方程，用GraphPad Prism 6.0计算IC 50值。每个实验一式两份进行并重复至少三次。 |
| Animal Experiment | 小鼠：(1)8至10周龄雌性SCID /米色小鼠静脉注射每只小鼠5×106个H3122细胞，当平均肿瘤大小达到300mm3时，随机选择治疗组(n = 10)(零日)。治疗以10mL / kg剂量体积口服给药连续21天。每周测量皮下肿瘤两次或三次。使用公式(L×W2)/ 2计算肿瘤体积(以mm 3计)。当肿瘤达到宿主体重的10％时，通过CO 2窒息使动物安乐死。(2)8至10周龄雌性SCID /米色小鼠皮下注射每只小鼠2.5×106个Karpas-299细胞，当平均肿瘤大小达到约180mm3时，随机选择治疗组(n = 10)(第零天)。以10mL / kg剂量体积连续14天口服给药。如针对H3122模型所述测量和计算肿瘤体积。 |
| Kinase Experiment | 进行289种激酶的体外HotSpotSM激酶谱分析。该测定在10μM[33P] -ATP存在下进行，使用浓度范围为0.05nM至1μM的布立替尼。 |
| Data Literature Source | [1]. Zhang S，et al. The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models. Clin Cancer Res. 2016 Nov 15;22(22):5527-5538 [2]. Huang WS，et al. Discovery of Brigatinib (AP26113)，a Phosphine Oxide-Containing，Potent，Orally Active Inhibitor of Anaplastic Lymphoma Kinase. J Med Chem. 2016 May 26;59(10):4948-64. [3]. Siaw JT，et al. Brigatinib，an anaplastic lymphoma kinase inhibitor，abrogates activity and growth in ALK-positive neuroblastoma cells，Drosophila and mice. Oncotarget. 2016 May 17;7(20):29011-22 |
| Unit | Bottle |
| Specification | 5mg 10mg 50mg 100mg |
是一种有效的、选择性的ALK抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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