| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| L408619-1ml |
1ml |
现货  |
|
| 英文别名 | N-(4-(3-fluorobenzyloxy)-3-chlorophenyl)-6-(5-((2-(methylsulfonyl)ethylamino)methyl)furan-2-yl)quinazolin-4-amine,di4-methylbenzenesulfonate |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | Lapatinib (GW-572016) Ditosylate |
| 生化机理 | 拉帕替尼（GW-572016）二对甲苯磺酸盐是一种强效的表皮生长因子受体（EGFR）和表皮生长因子受体（ErbB2）抑制剂，在无细胞实验中的 IC50 分别为 10.8 和 9.2 nM。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 产品介绍 |
Lapatinib (GW-572016) Ditosylate是一种有效的EGFR和ErbB2抑制剂，IC50分别为10.8和9.2 nM。 Information Lapatinib (GW-572016) Ditosylate is a potentEGFRandErbB2inhibitor withIC50of 10.8 and 9.2 nM in cell-free assays, respectively. Lapatinib Ditosylate weakly inhibits the activity of ErbB4 with IC50 of 367 nM, and displays >300-fold selectivity for EGFR and ErbB2 over other kinases such as c-Src, c-Raf, MEK, ERK, c-Fms, CDK1, CDK2, p38, Tie-2, and VEGFR2. Lapatinib Ditosylate significantly inhibits receptor autophosphorylation of EGFR and ErbB2 in a dose-dependent manner with IC50 of 170 nM and 80 nM, respectively in HN5 cells; as well as 210 nM and 60 nM, respectively in BT474 cells. Unlike OSI-774 and Iressa (ZD1839) which preferentially inhibit the growth of the EGFR-overexpressing cells, Lapatinib Ditosylate inhibits the growth of both EGFR- and ErbB2-overexpressing cells. Lapatinib Ditosylate displays higher inhibitory activity against EGFR- or ErbB2-overexpressing cells with IC50 of 0.09-0.21 μM, compared with cells expressing low levels of EGFR or ErbB2 with IC50 of 3-12 μM, and exhibits ~100-fold selectivity over the normal fibroblast cells. Lapatinib Ditosylate potently inhibits the outgrowth of EGFR-overexpressing HN5 and A-431 cells, as well as ErbB2-overexpressing BT474 and N87 cells, and significantly induces G1 arrest of HN5 cells and apoptosis of BT474 cells, which are associated with inhibition of AKT phosphorylation. In vivo Oral administration of Lapatinib Ditosylate (~100 mg/kg) twice daily significantly inhibits the growth of BT474 and HN5 xenografts in a dose-dependent manner. cell lines： Concentrations：Dissolved in DMSO, final concentrations ~100 μM Incubation Time：72 hours Powder Purity:≥99% |
| EC号 | 642-915-3, 879-201-8 |
|---|---|
| Isomeric SMILES | CC1=CC=C(C=C1)S(=O)(=O)O.CC1=CC=C(C=C1)S(=O)(=O)O.CS(=O)(=O)CCNCC1=CC=C(O1)C2=CC3=C(C=C2)N=CN=C3NC4=CC(=C(C=C4)OCC5=CC(=CC=C5)F)Cl |
| 关联CAS | 388082-78-8,388082-77-7 |
| MeSH Entry Terms | GW 282974X;GW 572016;GW-282974X;GW-572016;GW282974X;GW572016;lapatinib;lapatinib ditosylate;N-(3-chloro-4-(((3-fluorobenzyl)oxy)phenyl)-6-(5-(((2-methylsulfonyl)ethyl)amino)methyl) -2-furyl)-4-quinazolinamine;Tykerb |
| 分子量 | 925.46 |
| Reaxy-Rn | 11608649 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11608649&ln= |
| 溶解性 | Solubility (25°C) In vitro 5%TFA 3.04 mg/mL (11.95 mM); DMSO: 0.1 mg/mL (0.39 mM); Water: Insoluble; |
|---|
| 象形图 | GHS08 |
|---|---|
| 信号词 | Danger |
| 危险声明 |
H373: 通过长时间或反复暴露对器官造成损害 H413: 可能对水生生物造成长期的有害影响 H372: 通过长时间或反复暴露对器官造成损害 H360: 可能损害生育力或未出生的孩子 H362: 可能对母乳喂养的孩子造成伤害 |
| 预防措施声明 |
P273: 避免释放到环境中。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P263: 避免在怀孕期间/哺乳期间接触。 P203: 使用前，获取、阅读并遵守所有安全说明。 P318: 如果暴露或担心，请就医。 P319: 如果你感到不适，请寻求医疗帮助。 |
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