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Paclitaxel

SKU: orb1225286

Description

Paclitaxel is a novel antineoplastic agent, which was discovered in a screen of extracts of thousands of plants and natural products for antineoplastic activity by a National Y Institute program. Alought it functions as a mitotic inhibitor like vinca alkaloids, paclitaxel promotes the polymerization of tubulin instead of inducing the disassembly of microtubules, which inhibits the microtubules disassembly and promotes the formation of excessively stable, dysfunctional microtubules. Paclitaxel has exhibited antitumor activity against a broad spectrum of human Ys, including ovarian, breast, head and neck, and lung Y, in a large number of studies.(In Vitro):Paclitaxel (20 nM; 48 hours) induces programmed cell death and exists a block at the G2/M phase of the cell cycle.Paclitaxel (20 nM; 48 hours) induces a consistent increase in the level of p53.(In Vivo):Paclitaxel (1-20 mg/kg; i.p.; 1 time/2 days for five cycles) obviously induces liver metastases at the low-Paclitaxel group with little influence on primary tumor growth.

Research Area

Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number33069-62-4
MW853.92
Purity>98% (HPLC)
FormulaC47H51NO14
SMILESO=C1[C@H](OC(C)=O)C(C2(C)C)=C(C)[C@@H](OC([C@H](O)[C@@H](NC(C3=CC=CC=C3)=O)C4=CC=CC=C4)=O)C[C@@]2(O)[C@@H](OC(C5=CC=CC=C5)=O)[C@@]6([H])[C@@]1(C)[C@@H](O)C[C@@]7([H])OC[C@]76OC(C)=O
TargetMicrotubule/Tubulin
SolubilityEthanol: 18 mg/mL (21.07 mM); DMSO: 171 mg/mL (200.25 mM)

Bioactivity

In Vivo
Animal model: MDA-231 xenograft-bearing mice. Dosage: 1, 20 mg/kg. Administration: Intraperitoneal injection; five cycles (1 time/2 days). Result: Liver metastases were obviously induced in the low-PTX (1 mg/kg) group with little influence on primary tumor growth compared with high-PTX group.
In Vitro
Apoptosis Analysis Cell line: MCF-7, MDA-MB-231 cells. Concentration: 20 nM. Incubation time: 48 hours. Result: Induced programmed cell death. Cell Cycle Analysis Cell line: MCF-7, MDA-MB-231 cells. Concentration: 20 nM. Incubation time: 48 hours. Result: > 60% of MCF-7 cells and 50% of MDA-MB-231 cells were in the G2/M phase following 24 h treament. Western blot analysis. Cell line: MCF-7 cells (harboring wild-type p53 ). Concentration: 20 nM. Incubation time: 48 hours. Result: Induced a consistent increase in the level of p53.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

NSC 125973

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Paclitaxel (orb1225286)

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