Canertinib
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Cat.No：IC1740 Solarbio
CAS：267243-28-7
Storage：Powder:2-8℃，2 years
Purity：≥98%
Appearance：Light yellow to yellow Solid
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> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Angiogenesis > Canertinib
Product Information
| CAS | 267243-28-7 |
| Name | Canertinib |
| Molecular Formula | C24H25ClFN5O3 |
| Molecular Weight | 485.94 |
| Solubility | Soluble in DMSO ≥0.1mg/mL(Need ultrasonic) |
| Purity | ≥98% |
| Appearance | Light yellow to yellow Solid |
| Storage | Powder:2-8℃，2 years |
| EC | EINECS 1308068-626-2 |
| MDL | MFCD09837878 |
| SMILES | O=C(NC1=C(C=C2C(C(NC3=CC=C(C(Cl)=C3)F)=NC=N2)=C1)OCCCN4CCOCC4)C=C |
| Target Point | EGFR;ErbB2 |
| Passage | Angiogenesis; Protein Tyrosine Kinase/RTK; JAK/STAT Signaling |
| Background | Canertinib is a potent, irreversible EGFR inhibitor. |
| Biological Activity | Canertinib 是有效地，不可逆的 EGFR 抑制剂；抑制细胞 EGFR 和 ErbB2 自身磷酸化的 IC50 值分别为7.4和9 nM[1-2]。 |
| IC50 | EGFR:7.4nM ErbB2:9nM [1-2] |
| In Vitro | Canertinib以剂量依赖性方式显著抑制培养的黑素瘤细胞RaH3和RaH5的生长。 IC50约为0.8μM，并且5μM两种细胞系在治疗72小时内完全生长停滞。用1μMCanertinib孵育指数生长的RaH3和RaH5在处理24小时内将细胞积聚在细胞周期的G1期而不诱导细胞凋亡。 1μMCanertinib抑制ErbB1-3受体磷酸化，伴随着两种细胞系中Akt-，Erk1/2-和Stat3活性的降低[2]。 |
| In Vivo | Canertinib显示出优异的体内抗肿瘤活性，使口服给药后A431异种移植物的生长延迟超过50天[1]。通过ip注射40mg/kg /天的canertinib显著抑制裸鼠中人恶性黑素瘤异种移植物RaH3和RaH5的生长(图4)。对黑素瘤异种移植物的抗增殖作用在治疗后4天内已经可见，并且在整个治疗期间进一步增加，如通过肿瘤体积的差异所观察到的，在治疗的18天内达到统计学显著性[2]。 |
| Cell Experiment | 用递增浓度(0-10μM)的Canertinib处理RaH3和RaH5细胞72小时。将细胞悬浮在缓冲液中并计数[2]。 |
| Animal Experiment | 小鼠：当肿瘤显示可靠的生长时，Canertinib治疗开始。将小鼠随机分为对照组和治疗组。在canertinib处理的RaH3组(n = 4)和RaH5组(n = 7)中，每只小鼠每周5天在0.1ml 0.15M NaCl中腹膜内注射1.2mg卡培替尼(40mg/kg /天)。对照RaH3(n = 3)和RaH5(n = 7)小鼠仅根据相同的方案接受ip注射载体。在治疗期结束时，通过颈椎脱位处死小鼠，然后取出肿瘤并称重[2]。 |
| Data Literature Source | [1]. Smaill JB，et al. Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3，2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions. J Med Chem. 2000 Apr 6;43(7):1380-97. [2]. Djerf Severinsson EA，et al. The pan-ErbB receptor tyrosine kinase inhibitor canertinib promotes apoptosis of malignant melanoma in vitro and displays anti-tumor activity in vivo. Biochem Biophys Res Commun. 2011 Oct 28;414(3):563-8 |
| Unit | Bottle |
| Specification | 10mg 50mg |
是有效地，不可逆的 EGFR 抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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