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CAS No.: 388082-78-8

Lapatinib ditosylate monohydrate/二甲苯磺酸拉帕替尼 Catalog No. CSN12862

Synonyms: GW572016 ditosylate monohydrate;GW2016 ditosylate monohydrate;二甲苯磺酸拉帕替尼

Lapatinib Ditosylate Hydrate inhibits EGFR and ErbB2 with IC50 of 10.8 nM and 9.2 nM.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 EGFR

IC50:10.8nM HER2

IC50:9.2nM
描述EGFR (epidermal growth factor receptor) family consists of four members that belong to the ErbB lineage of proteins (ErbB1–4) with an external domain that binds activating ligands, such as EGF, and is overexpressed in a significant percentage of carcinomas and contributes to the malignant phenotype. Upon activation, EGFR phosphorylates both the receptor itself and a variety of “effector” protein. Lapatinib Ditosylate Hydrate is the ditosylate hydrate form of Lapatinib. Lapatinib is a dual inhibitor of both EGFR and ErbB2 with IC50 values of 10.8nM and 9.2nM (measured by kinase activity), respectively, 300-fold selective over other kinases tested except for ErbB-4 (IC50=367nM). Treatment with Lapatinib for 6h inhibited receptor autophosphorylation of EGFR and ErbB-2, as well as phosphorylation of serine-473 of AKT, the key signal transduction mediator, in a dose-responsive manner at concentration ranged from 0.03 to 10μM in BT474 and HN5 cell lines. Lapatinib showed growth inhibition with IC50 values ranged from 0.09-12μM in EGFR-overexpressing cell lines HN5 and A-431, the ErbB-2-overexpressing cell lines BT474, N87 and CaLu-3,as well as tumor cell lines expressing low levels of EGFR and ErbB-2, MCF-7 and T47D cells. Treatment with 1 and 10μM Lapatinib resulted in induction of G1 arrest and increased number of cells with sub-2N DNA content, consistent with cell death by an apoptotic mechanism, in EGFR-overexpressing cell line, HN5, and BT474 cells. Complete inhibition of tumor growth was seen at dose of 100mg/kg, orally, twice daily, in BT474 and HN5 human tumor xenografts.

动物研究

剂量

Rat: 100 mg/kg - 300 mg/kg^[3] (p.o.) Mice: 100 mg/kg^[4] (p.o.), 50 mg/kg^[5] (p.o.)

给药途径

p.o.

动物药代数据

Animal	Mice^[6]	Rats^[6]	Dogs^[6]
Dose	10 mg/kg	10 mg/kg	10 mg/kg
Administration	i.v. or p.o.	i.v. or p.o.	i.v. or p.o.
F	50.0% (p.o.)	24.0 ± 11.6% (p.o.)	41.9 ± 6.06% (p.o.)
T_1/2	5.69 h (i.v.) 1.99 h (p.o.)	12.3 ± 8.24 h (i.v.) 3.91 ± 3.98 h (p.o.)	5.85 ± 0.17 h (i.v.) 3.27 ± 1.18 h (p.o.)
T_max	0.50 h (i.v.) 0.50 h (p.o.)	0.08 h (i.v.) 0.50 - 1.00 h (p.o.)	0.08 h (i.v.) 4.00 h (p.o.)
CL	48.0 ml/min/kg (i.v.)	48.8 ± 14.3 ml/min/kg (i.v.)	12.2 ± 2.83 ml/min/kg (i.v.)
C_max	942 ng/ml (i.v.) 504 ng/ml (p.o.)	4557 ± 1210 ng/ml (i.v.) 288 ± 224 ng/ml (p.o.)	3793 ± 167 ng/ml (i.v.) 555 ± 15.1 ng/ml (p.o.)
AUC_∞	3469 ng·h/ml (i.v.) 1735 ng·h/ml (p.o.)	3596 ± 924 ng·h/ml (i.v.) 861 ± 420 ng·h/ml (p.o.)	14087 ± 3094 ng·h/ml (i.v.) 5916 ± 852 ng·h/ml (p.o.)
Vss	9.55 L/kg (i.v.)	6.16 ± 1.95 L/kg (i.v.)	5.70 ± 1.03 L/kg (i.v.)

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.0599 mL
- 5.2996 mL
- 10.5991 mL
- 5 mM
- 0.2120 mL
- 1.0599 mL
- 2.1198 mL
- 10 mM
- 0.1060 mL
- 0.5300 mL
- 1.0599 mL

技术信息

CAS号

388082-78-8

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C43H44ClFN4O11S3

运输

蓝冰

分子量

943.48

别名

GW572016 ditosylate monohydrate;GW2016 ditosylate monohydrate;二甲苯磺酸拉帕替尼;拉帕替尼二甲苯磺酸盐水合物

溶解度

DMSO	100.0 mg/mL (106.0 mM)

动物实验配方

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靶点	Description	IC50
EGFR		IC50:10.8nM
HER2		IC50:9.2nM

Lapatinib ditosylate monohydrate/二甲苯磺酸拉帕替尼 Catalog No. CSN12862

靶点选择性

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