Paclitaxel Inhibitor CAS No. 33069-62-4

Cat. No.	Name	Size	Price	Add Cart
KI0287	Paclitaxel	10 mg	$112
KI0287	Paclitaxel	25 mg	$236

Chemical Characteristic

Product Name	Paclitaxel
Synonyms	Taxol
CAS No.	33069-62-4
Molecular Weight	853.91
Formula	C₄₇H₅₁NO₁₄
Chemical Name	Benzenepropanoic acid, ?-(benzoylamino)-?-hydroxy-, (2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-6,12b-bis(acetyloxy)-12-(benzoyloxy)-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-4,11-dihydroxy-4a,8,13,13-tetramethyl-5-oxo-7,11-methano-1H-cyclodeca[3,4]benz[1,2-b
Smiles	O=C(N[C@H]([C@H](C(O[C@H]1C[C@]2(O)C(C)(C)C([C@@H](OC(C)=O)C([C@@]3(C)[C@]([C@@](CO4)(OC(C)=O)[C@H]4C[C@@H]3O)([H])[C@@H]2OC(C5=CC=CC=C5)=O)=O)=C1C)=O)O)C6=CC=CC=C6)C7=CC=CC=C7
Chemical Structure
Documents	HPLC MS COA

Biological activities

Paclitaxel is a mitotic inhibitor that targets tubulin. Paclitaxel can cause cells defects in mitotic spindle assembly, chromosome segregation, and cell division. Paclitaxel stabilizes the microtubule polymer and protects it from disassembly. Paclitaxel blocks progression of mitosis, and prolongs activation of the mitotic checkpoint triggers apoptosis or reversion to the G-phase of the cell cycle without cell division.[1,2] The median IC50 values of paclitaxel for the non-small cell lung cancer (NSCLC) cell lines are >32 µM, 9.4 µM and 0.027 µM at exposure durations of 3, 24, and 120 hours, respectively. The median IC50 values of paclitaxel for 14 small cell lung cancer (SCLC) cell lines are >32 µM, 25 µM and 5 µM, respectively.^[3] Paclitaxel has an IC50 value of 10 nM on paclitaxel-resistant human prostate carcinoma (Pac-10) cells and an IC50 value of 2 nM on human prostate carcinoma (DU-145) cells.^[4] In HeLa cells, 8 nM paclitaxel half-maximally blocks mitosis, whereas there is no increase in microtubule-polymer mass below 10 nM paclitaxel. In addition, 80 nM paclitaxel half-maximally increases the polymer mass.^[5] In nude mice bearing 1A9 ovarian carcinoma xenograft, paclitaxel (i.v. injection; 60 mg/kg) inhibits tumor growth in all the mice with a >50% reduction of the tumor mass (TR_{50) in half of them. 24 hours after paclitaxel (60 mg/kg) administration, gene expression is altered and affected genes involve in various biological functions including cell cycle regulation and cell proliferation, apoptosis, signal transduction and transcriptional regulation, fatty acid biosynthesis and sterol metabolism, and IFN-mediated signaling.^[6]}

References

[1] Bharadwaj R, et al. The spindle checkpoint, aneuploidy, and cancer. Oncogene. 2004, 23(11): 2016-2027. [2] Brito DA, et al. Microtubules do not promote mitotic slippage when the spindle assembly checkpoint cannot be satisfied. J Cell Biol. 2008, 182(4): 623-629. [3] Georgiadis MS, et al. Paclitaxel cytotoxicity against human lung cancer cell lines increases with prolonged exposure durations. Clin Cancer Res. 1997, 3(3):449-454. [4] Ranganathan S, et al. Altered beta-tubulin isotype expression in paclitaxel-resistant human prostate carcinoma cells. Br J Cancer. 1998, 77(4): 562-566. [5] Jordan MA, et al. Mechanism of mitotic block and inhibition of cell proliferation by taxol at low concentrations. Proc Natl Acad Sci U S A. 1993, 90(20): 9552-9556. [6] Bani MR, et al. Gene expression correlating with response to paclitaxel in ovarian carcinoma xenografts. Mol Cancer Ther. 2004, 3(2): 111-121.

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