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Docetaxel Chemical Structure
|Product name: Docetaxel|
|Cat. No.: HY-B0011|
Docetaxel(Taxotere), an analog of taxol, is an inhibitor of depolymerisation of microtubules through binding to stabilized microtubules.
in vitro: IC50 concentrations (reducing survival by 50%) ranged from 0.13-3.3 ng/ml, with three neuroblastoma lines proving most sensitive and three breast and two colon carcinoma lines showing least sensitivity . Docetaxel was shown to promote the assembly of microtubule protein without GTP in vitro, but no inhibitory effect on DNA, RNA and protein synthesis . Gene expression changes induced by paclitaxel treatment were mainly enriched in actin cytoskeleton (ACTC1, MYL2 and MYH2), tyrosine-protein kinases (ERRB4, KIT and TIE1) and focal adhesion pathway (MYL2, IGF1 and FLT1), while the expression alterations responding to docetaxel were highly co-related to cell surface receptor linked signal transduction (SHH, DRD5 and ADM2), cytokine-cytokine receptor interaction (IL1A and IL6) and cell cycleregulation (CCNB1, CCNE2 and PCNA) .
in vivo: The patients, between 15 and 80 years old with performance status (PS) of 0-2, received at least two cycles of docetaxel 60 mg m-2 intravenously at 3-4 week intervals . Intestinal damage after repeated dosing of docetaxel (20 mg/kg) for 3 weeks was more severe at 14HALO than at 2HALO (hours after light on). The intestinal protein expressions of Wee1, phosphorylated CDK1, and cleaved Caspase-3 were higher in the 14HALO group than in the 2HALO group, while that of survivin was lower in the 14HALO group .
Toxicity: Twenty-five patients were enrolled. Overall, 13/25 (52 %, 95 % CI 34-70) completed 4 cycles, and 19/25 (76 %, 95 % CI 60-87) completed ≥3 cycles. Twenty of 25 patients (80 %) experienced a Grade 3 or 4 adverse event .
|M.Wt||807.88||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO: ≥ 35 mg/mL
|1 mg||5 mg||10 mg|
|1 mM||1.2378 mL||6.1890 mL||12.3781 mL|
|5 mM||0.2476 mL||1.2378 mL||2.4756 mL|
|10 mM||0.1238 mL||0.6189 mL||1.2378 mL|
|Product Name||Sponsor Only||Condition||Start Date||End Date||Phase||Last Change Date|
|Docetaxel||Sanofi||Hormone refractory prostate cancer||31-JAN-06||Phase 4||15-JUN-10|
|Hoffmann-La Roche Inc||Breast tumor||31-AUG-05||31-JUL-09||Phase 4||16-AUG-11|
|Spanish Breast Cancer Research Group||Metastatic breast cancer||31-OCT-02||01-DEC-06||Phase 4||25-OCT-13|
|Simcere Pharmaceutical Group||Non-small-cell lung cancer||31-OCT-08||31-OCT-10||Phase 4||23-OCT-13|
|Hoffmann-La Roche AG||Breast tumor||12-JUL-04||Phase 4||13-SEP-13|
10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel derivative with improved pharmacological features and higher water solubility.
10-Oxo Docetaxel(Docetaxel Impurity) is a novel taxoid having remarkable anti-tumor properties and a Docetaxel intermediate.
2-methoxyestradiol (2ME2; NSC-659853) is a natural metabolite of estrogen that is known to inhibit HIF-1 alpha with an IC50 of 0.71 (plusmn) 0.11 (mu)M for the inhibition of BPAEC migration.
4(acute)-Demethylepipodophyllotoxin(4(acute)-DMEP) is a key intermediate compound for the preparation of podophyllotoxin-type anti-cancer drugs; a potent inhibitor of microtubule assembly.
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