Cabazitaxel Inhibitor CAS No. 183133-96-2

Cat. No.	Name	Size	Price
KI0091	Cabazitaxel	5 mg	$194.4
	Cabazitaxel	10 mg	$340.2
	Cabazitaxel	100 mg	$640
	Cabazitaxel	200 mg	$1200

Chemical Characteristic

Product Name	Cabazitaxel
Synonyms	Jevtana, XRP6258
CAS No.	183133-96-2
Molecular Weight	835.93
Formula	C₄₅H₅₇NO₁₄
Chemical Name	Benzenepropanoic acid, ?-[[(1,1-dimethylethoxy)carbonyl]amino]-?-hydroxy-, (2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-(acetyloxy)-12-(benzoyloxy)-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-11-hydroxy-4,6-dimethoxy-4a,8,13,13-tetramethyl-5-oxo-7,11-methano
Smiles	CC(C)(C)OC(=O)N[C@@H](c1ccccc1)[C@H](C(=O)OC1C[C@@]2(C(C(=C1C)[C@H](C(=O)[C@]1([C@@H]([C@@H]2OC(=O)c2ccccc2)[C@]2(C(C[C@@H]1OC)OC2)OC(=O)C)C)OC)(C)C)O)O
Chemical Structure

Biological activities

Cabazitaxel is a semi-synthetic derivative of a natural taxoid. Cabazitaxel is a microtubule inhibitor. Cabazitaxel is used for the treatment of hormone-refractory prostate cancer. In four cell lines P388 (lymphoblastic leukemia), HL60 (promyelocytic leukemia), KB (cervical adenocarcinoma), and Calc18 (breast carcinoma), cytotoxicity is noted with relatively low cabazitaxel concentrations (IC50 = 3-29 ng/mL).^[1] Besides, cabazitaxel suppresses proliferation and induced G2M arrest and apoptosis in both head and neck squamous cell carcinoma cell (HNSCC) line HN30 and HN12. Cabazitaxel and docetaxel produces similar alteration in the expression of cell cycle regulators, such as cyclin A and cyclin B1. Cabazitaxel decreases the expression of E2F and EGFR in HNSCC cells. Furthermore, cabazitaxel induces a greater level of bcl2 phosphorylation than docetaxel in HN12 cell line.^[2] In murine tumor xenografts (colon C38 and pancreas P03), cabazitaxel elicites complete tumor regressions. Notably, in cell lines resistant to a variety of other cytotoxic agents (ie, anthracyclines, vinca alkaloids, and the older taxanes), cabazitaxel is noted to still induce tumor regression. In 3 human colorectal cell lines (HCT-116, HCT-8, and HT-29), cabazitaxel has high antitumor activity. In lung models, dosing at the total highest nontoxic dose (THNTD, 36 mg/kg) yields 2.7 log cell kill (LCK) in the NCI-H460 cell line, and 2.2 LCK in the A549 cell line. In addition, cabazitaxel treatment achieves long-term tumor-free survival (exceeding 133 days) and complete tumor regression in pancreatic xenografts (MIA PaCa-2), head and neck xenografts (SR475), and prostate xenografts (DU145, a cell line that represents a hormone-resistant entity established from a prostate cancer brain metastasis). Furthermore, in orthotopic models, cabazitaxel leads to complete tumor regression in 4 out of 10 U251 tumors.^[1]

References

[1] Pal SK, et al. Critical appraisal of cabazitaxel in the management of advanced prostate cancer. Clin Interv Aging. 2010,5: 395-402. [2] Yoo GH, et al. XRP6258-induced gene expression patterns in head and neck cancer carcinoma. Laryngoscope. 2010, 120(6): 1114-1119.

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