CP-724714
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Cat.No：IC1800 Solarbio
CAS：537705-08-1
Storage：Powder:2-8℃，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 > Angiogenesis > CP-724714
Product Information
| CAS | 537705-08-1 |
| Name | CP-724714 |
| Molecular Formula | C27H27N5O3 |
| Molecular Weight | 469.53 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| SMILES | O=C(OCC)NC/C=C/C1=CC2=C(NC3=CC=C(OC4=CC=C(C)N=C4)C(C)=C3)N=CN=C2C=C1 |
| Target Point | HER2 inhibitor |
| Passage | Angiogenesis; Protein Tyrosine Kinase/RTK |
| Background | CP-724714 is a potent and selective ErbB2 (HER2) tyrosine kinase inhibitor. |
| Biological Activity | CP-724714是一种有效的，选择性HER2/ErbB2抑制剂，IC50为10 nM，无细胞试验中比作用于EGFR，InsR，IRG-1R，PDGFR，VEGFR2，Abl，Src，c-Met等选择性高640多倍。[1] |
| In Vitro | CP-724，714明显选择性作用于EGFR，IC50为6.4 μM。CP-724，714作用于IR，IGF-1R，PDGFRβ，VGFR2，Abl，Src，c-Met，c-jun NH2端激酶(JNK)-2，JNK-3，ZAP-70，周期蛋白依赖激酶(Cdk)-2，和Cdk-5效果要低1000倍以上。CP-724，714作用于含erbB2激酶域的嵌合体，有效降低EGF诱导的自磷酸化，IC50为32 nM，但是作用于转染EGFR的NIH3T3细胞效果明显低很多。CP-724，714抑制erbB2增强的细胞，包括BT-474和SKBR3的增殖，IC50分别为0.25和0.95 μM。1 μM CP-724，714作用于BT-474细胞，诱导细胞在G1期累积，而在S期明显减少。[1]CP-724，714可能通过肝细胞性损伤和胆汁淤积机制表现出肝毒性。CP-724，714抑制牛胆酸(TC)进入表达人类胆盐输出泵的膜囊泡，IC50为16 μM，且抑制胆小管，MDR1的主要外排转运，IC50为~28 μM。[2] |
| In Vivo | CP-724，714按25 mg/kg剂量口服处理FRE-erbB2和BT-474 移植瘤，快速吸收，且引起肿瘤erbB2 受体磷酸化降低。CP-724，714作用于皮下注射FRE-erbB2移植瘤的小鼠，诱导凋亡，按50 mg/kg剂量处理则显示肿瘤生长抑制达50%，且不会引起体重减轻或死亡。CP-724，714作用于MDA-MB-453，MDA-MB-231，LoVo(结肠)，和Colo-205(结肠)移植瘤具有强抗癌活性。而且，CP-724，714按30或100 mg/kg剂量处理BT-474移植瘤，降低胞外信号调节激酶和Akt磷酸化。[1] |
| Cell Experiment | 细胞按每孔5~103个接种在24孔板上，重复2份。加入通过滴定6或者更多的从0.1 nM到 10 μM的稀释CP-724，714。对照组没有CP-724，714。细胞生长6到7天，计数存活细胞。 [1] |
| Animal Experiment | Animal Models: 携带FRE-erbB2 BT-474，MDA-MB-453，MDA-MB-231，LoVo(结肠)，和 Colo-205(结肠)移植瘤的雌性无胸腺CD-1 nu/nu鼠; Dosages: ~100 mg/kg; Administration: 口服处理[1] |
| Data Literature Source | [1] Jani JP，et al. Cancer Res，2007，67(20)，9887-9893. [2] Feng B，et al. Toxicol Sci，2009，108(2)，492-500. |
| Unit | Bottle |
| Specification | 5mg 10mg |
CP-724714是一种高效、选择性的 ErbB2 (HER2) 酪氨酸激酶抑制剂。
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.
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