Erlotinib Hydrochloride
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Cat.No：IE0670 Solarbio
CAS：183319-69-9
Storage：Powder:2-8℃，2 years
Purity：HPLC≥98%
Appearance：White to off-white Solid
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> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Angiogenesis > Erlotinib Hydrochloride
Product Information
| CAS | 183319-69-9 |
| Name | Erlotinib Hydrochloride |
| Molecular Formula | C22H23N3O4·HCl |
| Molecular Weight | 429.9 |
| Solubility | Soluble in DMSO ≥0.1mg/mL(Need ultrasonic) |
| Purity | HPLC≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years |
| EC | EINECS 620-491-0 |
| MDL | MFCD07781272 |
| SMILES | COCCOC1=CC2=NC=NC(NC3=CC=CC(C#C)=C3)=C2C=C1OCCOC.[H]Cl |
| Target Point | EGFR |
| Passage | Angiogenesis;Protein Tyrosine Kinase/RTK; JAK/STAT Signaling |
| Background | Erlotinib inhibits EGFR kinase. |
| Biological Activity | Erlotinib 抑制 EGFR 激酶的 IC50 为 2 nM。[1-4] |
| IC50 | EGFR:2nM [1-4] |
| In Vitro | Erlotinib强烈抑制DiFi细胞的增殖，对于8天的增殖试验，IC50为100 nM [1]。与单独的任一种药剂相比，B-DIM和Erlotinib(2μM)的组合导致BxPC-3细胞中集落形成的显著抑制。与单独使用任一种药物的细胞凋亡作用相比，B-DIM和Erlotinib(2μM)的组合仅在BxPC-3细胞中导致显著的细胞凋亡诱导[2]。 |
| In Vivo | Erlotinib(5 mg/kg)比较Bcrp1/Mdr1a/1b - / - 与WT小鼠(分别为7，419±1，720和4，957±1，735 ng * h/mL)后，AUC0-inf之间的差异有1.49倍有统计学意义。，P = 0.01)[3]。给博来霉素(BLM)治疗的大鼠施用Erlotinib(10mg/kg /天，或20mg/kg /天)显示在宏观发现，肺重量，组织病理学评分(肺病变密度)等指标中没有肺损伤的恶化。和肺纤维化评分)和肺羟脯氨酸(HyP)水平。结果表明，Erlotinib对大鼠BLM诱导的肺损伤没有任何加剧作用[4]。 |
| Cell Experiment | 为了测试用B-DIM，Erlotinib或其组合处理的细胞的活力，将BxPC-3和MIAPaCa细胞接种(每孔3，000-5，000)在96孔板中并在37℃温育过夜。最初测试B-DIM(10-50μM)和Erlotinib(1-5μM)的浓度范围。基于初始结果，选择B-DIM(20μM)和Erlotinib(2μM)的浓度用于所有测定。 B-DIM(20μM)，Erlotinib(2μM)和组合对BxPC-3和MIAPaCa细胞的作用在72小时后通过标准MTT测定法测定并重复三次。通过Tecan微孔板荧光计在595nm处测量颜色强度。 DMSO处理的细胞被认为是未处理的对照并且被指定为100％的值。除上述检测外，我们还进行了克隆形成试验，以评估治疗效果[2]。 |
| Animal Experiment | 用5mg/kgErlotinib对小鼠[3] Bcrp1/Mdr1a/1b - / - 和WT小鼠进行po或ip处理。假设药物吸收良好且生物利用度完全，选择ip给药。从侧尾静脉的尖端以三个系列进行取样。在第一系列期间，在注射后15分钟和0.5，1.5，5和10小时收集全血样品。基于该初始组的结果，两个后续系列的采样时间适应于注射后5和15分钟以及0.5，1.5，4和8小时。收集后，立即将血液样品离心，并将血浆储存在-20°C，直至进行高效液相色谱分析。大鼠[4]使用7周龄雄性Crl：CD(SD)大鼠(244-297g)。通过管饲法口服Erlotinib盐酸盐(10mg/kg和20mg/kg)处理动物。 |
| Kinase Experiment | 激酶反应在50μL50mM HEPES(pH 7.3)中进行，含有125 mM NaCl，24 mM MgCl 2，0.1 mMNa3VO4，20μMATP，1.6μg/ mL EGF和15 ng EGFR，从A431中亲和纯化细胞膜。加入DMSO中的化合物，使DMSO的最终浓度为2.5％。通过添加ATP引发磷酸化，并在室温下继续进行8mm，持续摇动。通过抽吸反应混合物终止激酶反应，并用洗涤缓冲液洗涤4次。通过用50μL每孔HRP-缀合的PY54抗磷酸酪氨酸抗体孵育25mim来测量磷酸化PGT，在封闭缓冲液(3％BSA和0.05％Tween 20的PBS溶液)中稀释至0.2μg/ mL。通过抽吸除去抗体，并用洗涤缓冲液洗涤板4次。通过添加每孔50μL的TMB微孔过氧化物酶底物来培养结肠信号，并通过添加0.09M硫酸(每孔50μL)来终止。通过测量450nm处的吸光度来估计磷酸酪氨酸。对照的信号通常为0.6-1.2吸光度单位，在没有AlP，EGFR或POT的孔中基本上没有背景，并且与孵育10毫米的时间成比例[1]。 |
| Data Literature Source | [1]. Moyer JD，et al. Induction of apoptosis and cell cycle arrest by CP-358，774，an inhibitor of epidermal growth factor receptor tyrosine kinase. Cancer Res. 1997 Nov 1;57(21):4838-48. [2]. Ali S，et al. Apoptosis-inducing effect of erlotinib is potentiated by 3，3'-diindolylmethane in vitro and in vivo using an orthotopic model of pancreatic cancer. Mol Cancer Ther，2008，7(6)，1708-1719. [3]. Marchetti S，et al. Effect of the ATP-binding cassette drug transporters ABCB1，ABCG2，and ABCC2 on erlotinib hydrochloride (Tarceva) disposition in in vitro and in vivo pharmacokinetic studies employing Bcrp1-/-/Mdr1a/1b-/- (triple-knockout) and wild-typ [4]. Adachi K，et al. Effects of erlotinib on lung injury induced by intratracheal administration of bleomycin (BLM) in rats. J Toxicol Sci. 2010 Aug;35(4):503-14 |
| Unit | Bottle |
| Specification | 100mg 500mg 1g |
Erlotinib 可以抑制 EGFR 激酶。
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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