Discodermolide (Synonyms: NVP-XAA-296; XAA 296)

目录号: HY-105409 一键复制产品信息: Data Sheet 产品使用指南
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技术支持

Discodermolide (NVP-XAA-296) 是一种强效的微管 (microtubule) 稳定剂，其 K_i 值为 0.4 μM。Discodermolide 能够稳定微管，诱导 G2 期或 M 期细胞周期阻滞和细胞凋亡 (apoptosis)，从而抑制癌细胞增殖。Discodermolide 可竞争性抑制 Paclitaxel (HY-B0015) 与微管蛋白聚合物的结合，并抑制 Paclitaxel 耐药细胞的生长。Discodermolide 可用于乳腺癌和结肠癌的研究。

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Discodermolide Chemical Structure

CAS No. : 127943-53-7

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生物活性
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参考文献

生物活性

Discodermolide (NVP-XAA-296) is a potent microtubule-stabilizing agent with a K_i of 0.4 μM. Discodermolide stabilizes microtubules, induces G2 or M phase cell cycle arrest and apoptosis, leading to inhibition of cancer cell proliferation. Discodermolide competitively inhibits the binding of Paclitaxel (HY-B0015) to tubulin polymers, and inhibits the growth of Paclitaxel-resistant cells. Discodermolide can be used for breast and colon cancer research^[1]^[2]^[3].

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A2780	IC₅₀	10 nM Compound: Discodermolide	Inhibitory concentration of compound required for exhibiting cytotoxic effect on human A2780 cells; no. of experiment=4 Inhibitory concentration of compound required for exhibiting cytotoxic effect on human A2780 cells; no. of experiment=4	[PMID: 15837302]
A2780 ADR	IC₅₀	100 nM Compound: Discodermolide	Inhibitory concentration measured in term of cytotoxicity against human A2780/AD10 cells Inhibitory concentration measured in term of cytotoxicity against human A2780/AD10 cells	[PMID: 15837302]
A549	IC₅₀	0.015 μM Compound: 1	Cytotoxicity against human A549 cells Cytotoxicity against human A549 cells	[PMID: 15165132]
A549	IC₅₀	1.8 nM Compound: 22	Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured for 72 hrs Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured for 72 hrs	[PMID: 33038665]
A549	IC₅₀	13.5 nM Compound: 1	Cytotoxicity against human A549 cells Cytotoxicity against human A549 cells	[PMID: 12444691]
A549	IC₅₀	13.5 nM Compound: 1	Cytotoxicity against human A549 cells Cytotoxicity against human A549 cells	[PMID: 12502323]
A549	IC₅₀	22 nM Compound: (+)-discodermolide	Inhibitory concentration (toxicity at 10-20 mg/kg dose) exhibited against A549 cell line in mouse Inhibitory concentration (toxicity at 10-20 mg/kg dose) exhibited against A549 cell line in mouse	[PMID: 15979874]
A549	IC₅₀	9.34 nM Compound: (+)-1, 1	Antiproliferative activity against human A549 cells after 72 hrs by SRB method Antiproliferative activity against human A549 cells after 72 hrs by SRB method	[PMID: 21870795]
ASPC1	IC₅₀	98 nM Compound: 3	Cytotoxicity against human AsPC1 cells after 72 hrs by MTT assay Cytotoxicity against human AsPC1 cells after 72 hrs by MTT assay	[PMID: 17336522]
ASPC1	IC₅₀	98 nM Compound: 3	Cytotoxicity against taxol-sensitive human AsPC1 cells after 72 hrs by MTT assay Cytotoxicity against taxol-sensitive human AsPC1 cells after 72 hrs by MTT assay	[PMID: 18951787]
ASPC1	IC₅₀	98 nM Compound: 4	Cytotoxicity against human AsPC1 cells after 72 hrs by MTT assay Cytotoxicity against human AsPC1 cells after 72 hrs by MTT assay	[PMID: 18081257]
DLD-1	IC₅₀	29 nM Compound: 3	Cytotoxicity against human DLD1 cells after 72 hrs by MTT assay Cytotoxicity against human DLD1 cells after 72 hrs by MTT assay	[PMID: 17336522]
DLD-1	IC₅₀	29 nM Compound: 3	Cytotoxicity against taxol-sensitive human DLD1 cells after 72 hrs by MTT assay Cytotoxicity against taxol-sensitive human DLD1 cells after 72 hrs by MTT assay	[PMID: 18951787]
DLD-1	IC₅₀	29 nM Compound: 4	Cytotoxicity against human DLD1 cells after 72 hrs by MTT assay Cytotoxicity against human DLD1 cells after 72 hrs by MTT assay	[PMID: 18081257]
MCF7	IC₅₀	0.0024 μM Compound: 1	Cytotoxicity against human MCF7 cells Cytotoxicity against human MCF7 cells	[PMID: 15165132]
MCF7	IC₅₀	28 nM Compound: (+)-discodermolide	Inhibitory concentration (toxicity at 10-20 mg/kg dose) exhibited against MCF-7 cell line in mouse Inhibitory concentration (toxicity at 10-20 mg/kg dose) exhibited against MCF-7 cell line in mouse	[PMID: 15979874]
MCF7	IC₅₀	7.98 nM Compound: (+)-1, 1	Antiproliferative activity against human MCF7 cells after 96 hrs by SRB method Antiproliferative activity against human MCF7 cells after 96 hrs by SRB method	[PMID: 21870795]
NCI	IC₅₀	160 nM Compound: 3	Cytotoxicity against human Taxol-adriamycin-resistant NCI cells after 72 hrs by MTT assay Cytotoxicity against human Taxol-adriamycin-resistant NCI cells after 72 hrs by MTT assay	[PMID: 17336522]
NCI/ADR-RES	IC₅₀	160 nM Compound: 3	Cytotoxicity against taxol-resistant human NCI/ADR-RES cells after 72 hrs by MTT assay Cytotoxicity against taxol-resistant human NCI/ADR-RES cells after 72 hrs by MTT assay	[PMID: 18951787]
P388	IC₅₀	0.033 μM Compound: 1	Cytotoxicity against mouse P388 cells Cytotoxicity against mouse P388 cells	[PMID: 15165132]
P388	IC₅₀	0.5 μg/mL Compound: 22	Antiproliferative activity against mouse P388 cells assessed as cell growth inhibition Antiproliferative activity against mouse P388 cells assessed as cell growth inhibition	[PMID: 33038665]
P388	IC₅₀	35 nM Compound: 1	Cytotoxicity against mouse P388 cells after 48 hrs by MTT assay Cytotoxicity against mouse P388 cells after 48 hrs by MTT assay	[PMID: 11429994]
P388	IC₅₀	35 nM Compound: 1	Cytotoxicity against mouse P388 cells after 48 hrs by MTT assay Cytotoxicity against mouse P388 cells after 48 hrs by MTT assay	[PMID: 12444691]
P388	IC₅₀	35 nM Compound: 1	Cytotoxicity against mouse P388 cells Cytotoxicity against mouse P388 cells	[PMID: 12502323]
P388	IC₅₀	35 nM Compound: 4	Cytotoxicity against mouse P388 cells by MTT assay Cytotoxicity against mouse P388 cells by MTT assay	[PMID: 18081257]
PANC-1	IC₅₀	0.049 μM Compound: 1	Cytotoxicity against human PANC1 cells Cytotoxicity against human PANC1 cells	[PMID: 15165132]
PANC-1	IC₅₀	59 nM Compound: 3	Cytotoxicity against human PANC1 cells after 72 hrs by MTT assay Cytotoxicity against human PANC1 cells after 72 hrs by MTT assay	[PMID: 17336522]
PANC-1	IC₅₀	59 nM Compound: 3	Cytotoxicity against taxol-sensitive human PANC1 cells after 72 hrs by MTT assay Cytotoxicity against taxol-sensitive human PANC1 cells after 72 hrs by MTT assay	[PMID: 18951787]
PANC-1	IC₅₀	59 nM Compound: 4	Cytotoxicity against human PANC1 cells after 72 hrs by MTT assay Cytotoxicity against human PANC1 cells after 72 hrs by MTT assay	[PMID: 18081257]
SK-OV-3	IC₅₀	21 nM Compound: (+)-discodermolide	Inhibitory concentration (toxicity at 10-20 mg/kg dose) exhibited against SKOV3 cell line in mouse Inhibitory concentration (toxicity at 10-20 mg/kg dose) exhibited against SKOV3 cell line in mouse	[PMID: 15979874]
SK-OV-3	IC₅₀	6.1 nM Compound: 22	Antiproliferative activity against human SK-OV-3 cells assessed as cell growth inhibition measured for 72 hrs Antiproliferative activity against human SK-OV-3 cells assessed as cell growth inhibition measured for 72 hrs	[PMID: 33038665]
Vero	IC₅₀	30 μM Compound: 1	Cytotoxicity against african green monkey Vero cells Cytotoxicity against african green monkey Vero cells	[PMID: 15165132]

分子量

593.79

Formula

C₃₃H₅₅NO₈

CAS 号

127943-53-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料

产品使用指南 (1538 KB)

参考文献

[1]. Altmann KH. Microtubule-stabilizing agents: a growing class of important anticancer drugs. Curr Opin Chem Biol. 2001 Aug;5(4):424-31. [Content Brief]

[2]. Kowalski RJ, et al. The microtubule-stabilizing agent discodermolide competitively inhibits the binding of paclitaxel (Taxol) to tubulin polymers, enhances tubulin nucleation reactions more potently than paclitaxel, and inhibits the growth of paclitaxel-resistant cells. Mol Pharmacol. 1997 Oct;52(4):613-22. [Content Brief]

[3]. Hung DT, et al. (+)-Discodermolide binds to microtubules in stoichiometric ratio to tubulin dimers, blocks taxol binding and results in mitotic arrest. Chem Biol. 1996 Apr;3(4):287-93. [Content Brief]

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量		浓度		体积		分子量 *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)	×	体积 _(start)	=	浓度 _(final)	×	体积 _(final)
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Discodermolide127943-53-7NVP-XAA-296 XAA 296XAA296XAA 296XAA-296Microtubule/TubulinApoptosismicrotubulePaclitaxeltubulin polymersPaclitaxel-resistant cellsbreast cancercolon cancerInhibitorinhibitorinhibit

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上海工商

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沪(浦)应急管危经许[2021]201709(QFYS)

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Discodermolide (Synonyms: NVP-XAA-296; XAA 296)

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Discodermolide 相关分类

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