VE-821
VE-821
CAS:1232410-49-9
分子式:C18H16N4O3S
分子量:368.4096
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Pharmacology
Afatinib acts as an irreversible covalent inhibitor of the receptor tyrosine kinases epidermal growth factor receptor (EGFR) and erbB-2 (HER2) used to treat metastatic non-small cell lung cancer (NSCLC) that has certain EGFR mutations.
Efficacy
| Animal Model | Administration | Dosage | Formulation | Description |
|---|---|---|---|---|
| Xenograft mice models of RPC-9 and H1975[1] | once daily, 5 days per week as a suspension by gavage | 10 mg/kg | 0.5 w/v (%) methyl cellulose | Afatinib significantly enhances mouse survival |
| C3H/HeN mice bearing xenografttumours[2] | Daily oral treatment for 7 days | 10 mg/kg | 0.5% methylcellulose [wt/vol] and 0.4% Tween 80 [vol/vol] in sterile water | Afatinib combined with Radiotherapydecreasestumour metabolism and inhibited tumourgrowth |
| H460/MX20 cell xenograft tumor model [3] | every 3 d × 6, PO | 20mg/kg | saline | Afatinib in combination with topotecan significantly decreased the sizes, weights and volumes of xenograft tumors |
| xenograft mouse model transplanted with HCT-15 cells (high-expression HER2) or MKN45 cells [4] | i.v. once every 3 days for 9 days | 5 mg/kg | Normal saline | Afatinib reducestumorgrowth in HER2-overexpressedxenografts |
| mice harbouringxenografts of ARK2[5] | oral gavage daily | 25 mg/kg | sterile water with 0.5% methylcellulose | Afatinib treatment results in tumour shrinkage or a markedly slower rate of tumour growth |
Pharmacokinetics and Pharmacodynamics
To be updated
Toxicity
To be updated
References
[1] Ninomiya T, et al. MolCancerTher, 2013, 12(5), 589-597.
[2] Tsai YC, et al. Eur J Cancer, 2013, 49(6), 1458-1466.
[3]Wang XK, et al. Oncotarget, 2014, 5(23), 11971-11985.
[4]Guan SS, et al. Oncotarget, 2014, 5(13), 4868-4880.
[5]Schwab CL, et al. Br J Cancer, 2014, 111(9), 1750-1756.
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