Thiocolchicine

目錄號(hào): HY-116852 純度: 99.77%: FAQs
Data Sheet SDS COA 產(chǎn)品使用指南技術(shù)支持

Thiocolchicine 是秋水仙堿 (HY-16569) 的衍生物，是一種有效的微管蛋白聚合 (tubulin polymerization) 抑制劑 (IC₅₀=2.5 μM)，競(jìng)爭(zhēng)性結(jié)合微管蛋白 (K_i=0.7 μM)。Thiocolchicine 可以作為 ADC 的毒素分子。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Thiocolchicine Chemical Structure

CAS No. : 2730-71-4

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3. 試用裝只面向終端客戶。

規(guī)格	價(jià)格	是否有貨
5 mg	￥500	In-stock
10 mg	￥800	In-stock
25 mg	￥1600	In-stock
50 mg	￥2600	In-stock
100 mg	￥4150	In-stock
200 mg		詢價(jià)
500 mg		詢價(jià)

or 大包裝詢價(jià)

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Customer Review

Other Forms of Thiocolchicine:

Thiocolchicine-d₃ In-stock

Thiocolchicine 相關(guān)產(chǎn)品

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•同靶點(diǎn)產(chǎn)品:

•同靶點(diǎn)蛋白產(chǎn)品:

生物活性
純度 & 產(chǎn)品資料
參考文獻(xiàn)

生物活性

Thiocolchicine, a derivative modified in the C Ring of Colchicine (HY-16569) with enhanced biological properties. Thiocolchicine is a potent inhibitor of tubulin polymerization (IC₅₀=2.5 μM) and competitively binds to tubulin with a K_i of 0.7 μM. Thiocolchicine induces cell apoptosis^[1]^[2]. Thiocolchicine can be used as an ADC cytotoxin in ADC technology.

細(xì)胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	ED₅₀	0.0019 μg/mL Compound: 2	Cytotoxicity against human A549 cells after 2 days Cytotoxicity against human A549 cells after 2 days	[PMID: 20542428]
A549	IC₅₀	0.5 μM Compound: 1	Cytotoxicity against human A549 cells after 24 hrs by MTS assay Cytotoxicity against human A549 cells after 24 hrs by MTS assay	[PMID: 19880222]
A549	IC₅₀	0.6 μM Compound: Thiocolchicine	Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay	[PMID: 27449957]
A549	IC₅₀	0.9 nM Compound: TCOLCH	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by SRB assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by SRB assay	[PMID: 34592435]
A549	IC₅₀	11.3 nM Compound: 2	Antiproliferative activity against human A549 cells incubated for 72 hrs by SRB assay Antiproliferative activity against human A549 cells incubated for 72 hrs by SRB assay	[PMID: 33465696]
A549	IC₅₀	72 nM Compound: 6	Antiproliferative activity against human A549 cells incubated for 36 hrs Antiproliferative activity against human A549 cells incubated for 36 hrs	[PMID: 32432867]
BALB/3T3	IC₅₀	137 nM Compound: 2	Antiproliferative activity against mouse BALB/3T3 cells incubated for 72 hrs by SRB assay Antiproliferative activity against mouse BALB/3T3 cells incubated for 72 hrs by SRB assay	[PMID: 33465696]
BALB/3T3	IC₅₀	9.6 nM Compound: TCOLCH	Cytotoxicity against mouse BALB/3T3 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Cytotoxicity against mouse BALB/3T3 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 34592435]
Caco-2	IC₅₀	0.5 μM Compound: 1	Cytotoxicity against human Caco-2 cells after 24 hrs by MTS assay Cytotoxicity against human Caco-2 cells after 24 hrs by MTS assay	[PMID: 19880222]
DU-145	ED₅₀	0.0012 μg/mL Compound: 2	Cytotoxicity against human DU145 cells after 2 days Cytotoxicity against human DU145 cells after 2 days	[PMID: 20542428]
H9	IC₅₀	0.0017 μM Compound: 9	Antiviral activity against HIV1 HTLV-3B in human H9 cells after 3 days by p24 antigen capture assay Antiviral activity against HIV1 HTLV-3B in human H9 cells after 3 days by p24 antigen capture assay	[PMID: 1919593]
HCT-8	ED₅₀	0.008 μg/mL Compound: 2	Cytotoxicity against human HCT8 cells after 2 days Cytotoxicity against human HCT8 cells after 2 days	[PMID: 20542428]
HCT-8	IC₅₀	15 nM Compound: 6	Antiproliferative activity against human HCT-8 cells incubated for 36 hrs Antiproliferative activity against human HCT-8 cells incubated for 36 hrs	[PMID: 32432867]
HepG2	IC₅₀	0.5 μM Compound: 1	Cytotoxicity against human HepG2 cells after 24 hrs by MTS assay Cytotoxicity against human HepG2 cells after 24 hrs by MTS assay	[PMID: 19880222]
IGROV-1	IC₅₀	0.012 μM Compound: 1	Antiproliferative activity against human IGROV1 cells assessed as growth inhibition after 72 hrs by Coulter counting analysis Antiproliferative activity against human IGROV1 cells assessed as growth inhibition after 72 hrs by Coulter counting analysis	[PMID: 19833515]
KB	ED₅₀	0.0008 μg/mL Compound: 2	Cytotoxicity against human KB cells after 2 days Cytotoxicity against human KB cells after 2 days	[PMID: 20542428]
KB	IC₅₀	0.04 nM Compound: 6	Antiproliferative activity against human KB cells incubated for 36 hrs Antiproliferative activity against human KB cells incubated for 36 hrs	[PMID: 32432867]
LoVo	IC₅₀	1 nM Compound: TCOLCH	Antiproliferative activity against human LoVo cells assessed as inhibition of cell proliferation incubated for 72 hrs by SRB assay Antiproliferative activity against human LoVo cells assessed as inhibition of cell proliferation incubated for 72 hrs by SRB assay	[PMID: 34592435]
LoVo	IC₅₀	21 nM Compound: 2	Antiproliferative activity against human LoVo cells incubated for 72 hrs by SRB assay Antiproliferative activity against human LoVo cells incubated for 72 hrs by SRB assay	[PMID: 33465696]
MCF7	IC₅₀	0.1 μM Compound: Thiocolchicine	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay	[PMID: 27449957]
MCF7	IC₅₀	1.1 nM Compound: TCOLCH	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by SRB assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by SRB assay	[PMID: 34592435]
MCF7	IC₅₀	400 nM Compound: 2	Anti tumor activity on human breast cancer cell line MDR-positive MCF-7 ADRr after 72 hours of treatment Anti tumor activity on human breast cancer cell line MDR-positive MCF-7 ADRr after 72 hours of treatment	[PMID: 10602712]
MCF7	IC₅₀	9.6 nM Compound: 2	Antiproliferative activity against human MCF-7 cells incubated for 72 hrs by SRB assay Antiproliferative activity against human MCF-7 cells incubated for 72 hrs by SRB assay	[PMID: 33465696]
MDA-MB-231	IC₅₀	0.1 μM Compound: Thiocolchicine	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay	[PMID: 27449957]
MDA-MB-231	IC₅₀	0.6 nM Compound: 2	Anti tumor activity on human breast cancer cell line MDR-negative MDA-MB 231 after 72 hours of treatment Anti tumor activity on human breast cancer cell line MDR-negative MDA-MB 231 after 72 hours of treatment	[PMID: 10602712]
MDA-MB-468	IC₅₀	0.2 μM Compound: Thiocolchicine	Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay	[PMID: 27449957]
P388	IC₅₀	5 nM Compound: 6	Antiproliferative activity against mouse P388 cells incubated for 36 hrs Antiproliferative activity against mouse P388 cells incubated for 36 hrs	[PMID: 32432867]
RPMI-7951	IC₅₀	0.024 nM Compound: 6	Antiproliferative activity against human RPMI-7951 cells incubated for 36 hrs Antiproliferative activity against human RPMI-7951 cells incubated for 36 hrs	[PMID: 32432867]
SK-BR-3	ED₅₀	0.0015 μg/mL Compound: 2	Cytotoxicity against human SKBR3 cells after 2 days Cytotoxicity against human SKBR3 cells after 2 days	[PMID: 20542428]
T47D	IC₅₀	4.1 μM Compound: Thiocolchicine	Antiproliferative activity against human T47D cells assessed as reduction in cell viability measured after 72 hrs by MTS assay Antiproliferative activity against human T47D cells assessed as reduction in cell viability measured after 72 hrs by MTS assay	[PMID: 27449957]
TE-671	IC₅₀	0.024 nM Compound: 6	Antiproliferative activity against human TE-671 cells incubated for 36 hrs Antiproliferative activity against human TE-671 cells incubated for 36 hrs	[PMID: 32432867]

體外研究
(In Vitro)

Thiocolchicine is against MCF-7, LoVo, LoVo/DX, A-549 and BALB/3T3 cells with IC₅₀ values of 0.01 μM, 0.021 μM, 0.398 μM, 0.011 μM and 0.114 μM, respectively^[3].
Thiocolchicine (1 nM-100 μM; 24-72 hours) shows a relationship between cell cycle blocking activity and growth inhibition in breast cancer cells. It inhibits cell proliferation of MDA-MB-231 and multidrug resistant (MDR) MCF-7 ADRr breast cancer cells with IC₅₀s of 0.6 nM and 400 nM, respectively, as well as MDR CEM-VBL leukemia cells (IC₅₀=50 nM)^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

415.50

Formula

C₂₂H₂₅NO₅S

CAS 號(hào)

2730-71-4

性狀

固體

顏色

Light yellow to green yellow

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性數(shù)據(jù)

細(xì)胞實(shí)驗(yàn)：

DMSO 中的溶解度 : 100 mg/mL (240.67 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

配制儲(chǔ)備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	2.4067 mL	12.0337 mL	24.0674 mL
5 mM	0.4813 mL	2.4067 mL	4.8135 mL
10 mM	0.2407 mL	1.2034 mL	2.4067 mL

查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

摩爾計(jì)算器
稀釋計(jì)算器

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥方式選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

方案一

請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.02 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水定容至 1 mL。
生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
方案二

請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.02 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液中，混合均勻。
2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。

動(dòng)物溶解方案計(jì)算器

請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只

由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量

請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：

DMSO +

Tween-80 +

Saline

如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。

方案所需 助溶劑 包括：DMSO，，均可在 MCE 網(wǎng)站選購。，Tween 80，均可在 MCE 網(wǎng)站選購。

計(jì)算結(jié)果

工作液所需濃度 : mg/mL

儲(chǔ)備液配制方法 : mg 藥物溶于 μL DMSO（母液濃度為 mg/mL）。

您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國技術(shù)支持聯(lián)系。

動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。

連續(xù)給藥周期超過半月以上，請(qǐng)謹(jǐn)慎選擇該方案。

請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱（超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。

純度 & 產(chǎn)品資料

純度: 99.77%

選擇批次：

Data Sheet (627 KB) SDS (251 KB)

COA (299 KB) HNMR (224 KB) LCMS (263 KB) OR (169 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻(xiàn)

[1]. Klaus M.Hahn, et al. Structural requirements for the binding of colchicine analogs to tubulin: the role of the C-10 substituent. Bioorganic & Medicinal Chemistry Letters.Volume 1, Issue 9, 1991, Pages 471-476

[2]. R De Vincenzo, et al. Antiproliferative Activity of Colchicine Analogues on MDR-positive and MDR-negative Human Cancer Cell Lines. Anticancer Drug Des. 1998 Jan;13(1):19-33. [Content Brief]

Thiocolchicine 相關(guān)分類

完整儲(chǔ)備液配制表

可選溶劑	濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.4067 mL	12.0337 mL	24.0674 mL	60.1685 mL
	5 mM	0.4813 mL	2.4067 mL	4.8135 mL	12.0337 mL
	10 mM	0.2407 mL	1.2034 mL	2.4067 mL	6.0168 mL
	15 mM	0.1604 mL	0.8022 mL	1.6045 mL	4.0112 mL
	20 mM	0.1203 mL	0.6017 mL	1.2034 mL	3.0084 mL
	25 mM	0.0963 mL	0.4813 mL	0.9627 mL	2.4067 mL
	30 mM	0.0802 mL	0.4011 mL	0.8022 mL	2.0056 mL
	40 mM	0.0602 mL	0.3008 mL	0.6017 mL	1.5042 mL
	50 mM	0.0481 mL	0.2407 mL	0.4813 mL	1.2034 mL
	60 mM	0.0401 mL	0.2006 mL	0.4011 mL	1.0028 mL
	80 mM	0.0301 mL	0.1504 mL	0.3008 mL	0.7521 mL
	100 mM	0.0241 mL	0.1203 mL	0.2407 mL	0.6017 mL

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:

Thiocolchicine2730-71-4Microtubule/TubulinApoptosisMCF-7LoVoLoVo/DXA-549BALB/3T3breastcancerleukemiaAnalogueMDR-positiveColchicineInhibitorinhibitorinhibit

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Thiocolchicine

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