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1.Basic Info:
Product Name:Capecitabine
CAS:154361-50-9
Appearance:White power
MF:C15H22FN3O6
Purity:99%
Storage:Stored in a clean,cool, dry area
Function:It is an orally-administered chemotherapeutic agent used in the treatment of metastatic breast and colorectal cancers.
2.Product Description:
Ceritinib (LDK378) is potent inhibitor against ALK with IC50 of 0.2 nM in cell-free assays, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively.
Ceritinib shows great anti-proliferative activity in Ba/F3-NPM-ALK and Karpas290 cells with IC50 of 26.0 nM and 22.8 nM, compared with IC50 of 319.5 nM and 2477 nM in Ba/F3-Tel-InsR and Ba/F3-WT cells.
Ceritinib is designed to reduce the possibility of forming reactive metabolites and shows undetectable levels of glutathione (GSH) adducts (<1%) in liver microsomes. Ceritinib has relatively good metabolic stability, with moderate CYP3A4 inhibition and hERG inhibition.
LDK378 exhibits low plasma clearance in animals (mouse, rat, dog and monkey) compared to liver blood flow, with the oral bioavailability of above 55% in mouse, rat, dog and monkey. Ceritinib induces a dose-dependent growth inhibition and tumor regression in the Karpas299 and H2228 rat xenograft models, with no body-weight loss.Ceritinib shows no impact on insulin levels or plasma glucose utilization in the mouse upon chronic dosing up to 100 mg/kg.
LDK378 exhibits low plasma clearance in animals (mouse, rat, dog and monkey) compared to liver blood flow, with the oral bioavailability of above 55% in mouse, rat, dog and monkey. Ceritinib induces a dose-dependent growth inhibition and tumor regression in the Karpas299 and H2228 rat xenograft models, with no body-weight loss.Ceritinib shows no impact on insulin levels or plasma glucose utilization in the mouse upon chronic dosing up to 100 mg/kg.
3.Product Application:
Capecitabine is a chemotherapy drug that usually given to treat cancer of the colon, rectum, breast,stomach, pancreas and gullet(oesophagus).
Capecitabine is a prodrug, that is enzymatically converted to 5-fluorouracil in the tumor, where it inhibits DNA synthesis and slows growth of tumor tissue. The activation of capecitabine follows a pathway with three enzymatic steps and two intermediary metabolites, 5'-deoxy-5-fluorocytidine (5'-DFCR) and 5'-deoxy-5-fluorouridine (5'-DFUR), to form 5-fluorouracil.
