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  1. Cell Cycle/DNA Damage Cytoskeleton Apoptosis Anti-infection
  2. Microtubule/Tubulin Apoptosis HPV
  3. Sabizabulin

Sabizabulin  (Synonyms: VERU-111; ABI-231)

目錄號(hào): HY-120599 純度: 99.00%
COA 產(chǎn)品使用指南 技術(shù)支持

VERU-111 (ABI-231) 是一種高效、口服可利用 α/β 微管蛋白 (tubulin) 抑制劑,具有很強(qiáng)的抗增殖活性,對(duì)黑素瘤和前列腺癌細(xì)胞系作用的平均 IC50 值為 5.2 nM。VERU-111 (ABI-231) 通過靶向 HPV E6 和 E7 抑制腫瘤生長(zhǎng)和轉(zhuǎn)移表型,有潛力用于前列腺癌的研究。

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Sabizabulin Chemical Structure

Sabizabulin Chemical Structure

CAS No. : 1332881-26-1

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Customer Review

Other Forms of Sabizabulin:

MCE 顧客使用本產(chǎn)品發(fā)表的 2 篇科研文獻(xiàn)

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

VERU-111 (ABI-231) is a potent and orally active α and β tubulin inhibitor, which displays strong antiproliferative activity, with an average IC50 of 5.2 nM against panels of melanoma and prostate cancer cell lines. VERU-111 (ABI-231) suppresses tumor growth and metastatic phenotypes of cervical cancer cells via targeting HPV E6 and E7, and has potential for the treatment of prostate cancer[1][2][3].

IC50 & Target

tubulin[1]

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
A-375 IC50
10.4 nM
Compound: ABI-231
Antiproliferative activity against human A375 cells measured after 72 hrs by MTS assay
Antiproliferative activity against human A375 cells measured after 72 hrs by MTS assay
[PMID: 31860298]
A-375 IC50
3.2 nM
Compound: 6a
Antiproliferative activity against human A375 cells after 48 hrs by SRB assay
Antiproliferative activity against human A375 cells after 48 hrs by SRB assay
[PMID: 22783954]
A-375 IC50
8.1 nM
Compound: VERU-111
Cytotoxicity in human A375 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
Cytotoxicity in human A375 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
[PMID: 30122035]
A-375 IC50
8.1 nM
Compound: ABI-231
Antiproliferative activity against human A375 cells after 72 hrs by MTT assay
Antiproliferative activity against human A375 cells after 72 hrs by MTT assay
[PMID: 31251599]
DU-145 IC50
3.9 nM
Compound: 6a
Antiproliferative activity against human DU145 cells after 48 hrs by SRB assay
Antiproliferative activity against human DU145 cells after 48 hrs by SRB assay
[PMID: 22783954]
LNCaP IC50
2.8 nM
Compound: 6a
Antiproliferative activity against human LNCAP cells after 48 hrs by SRB assay
Antiproliferative activity against human LNCAP cells after 48 hrs by SRB assay
[PMID: 22783954]
M14 IC50
5.6 nM
Compound: VERU-111
Cytotoxicity in human M14 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
Cytotoxicity in human M14 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
[PMID: 30122035]
M14 IC50
5.6 nM
Compound: ABI-231
Antiproliferative activity against human M14 cells after 72 hrs by MTT assay
Antiproliferative activity against human M14 cells after 72 hrs by MTT assay
[PMID: 31251599]
M14 IC50
8.9 nM
Compound: ABI-231
Antiproliferative activity against human M14 cells measured after 72 hrs by MTS assay
Antiproliferative activity against human M14 cells measured after 72 hrs by MTS assay
[PMID: 31860298]
MDA-MB-231 IC50
8.2 nM
Compound: ABI-231
Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by MTS assay
Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by MTS assay
[PMID: 31860298]
MDA-MB-453 IC50
13.6 nM
Compound: ABI-231
Antiproliferative activity against human MDA-MB-453 cells measured after 72 hrs by MTS assay
Antiproliferative activity against human MDA-MB-453 cells measured after 72 hrs by MTS assay
[PMID: 31860298]
PC-3 IC50
3.7 nM
Compound: 6a
Antiproliferative activity against human PC3 cells after 48 hrs by SRB assay
Antiproliferative activity against human PC3 cells after 48 hrs by SRB assay
[PMID: 22783954]
RPMI-7951 IC50
7.2 nM
Compound: VERU-111
Cytotoxicity in human RPMI7951 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
Cytotoxicity in human RPMI7951 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
[PMID: 30122035]
RPMI-7951 IC50
8.8 nM
Compound: ABI-231
Antiproliferative activity against human RPMI7951 cells measured after 72 hrs by MTS assay
Antiproliferative activity against human RPMI7951 cells measured after 72 hrs by MTS assay
[PMID: 31860298]
SK-BR-3 IC50
13.3 nM
Compound: ABI-231
Antiproliferative activity against human SK-BR-3 cells measured after 72 hrs by MTS assay
Antiproliferative activity against human SK-BR-3 cells measured after 72 hrs by MTS assay
[PMID: 31860298]
WM164 IC50
5.3 nM
Compound: 6a
Antiproliferative activity against human WM164 cells after 48 hrs by SRB assay
Antiproliferative activity against human WM164 cells after 48 hrs by SRB assay
[PMID: 22783954]
WM164 IC50
7.2 nM
Compound: ABI-231
Antiproliferative activity against human WM164 cells after 72 hrs by MTT assay
Antiproliferative activity against human WM164 cells after 72 hrs by MTT assay
[PMID: 31251599]
體外研究
(In Vitro)

VERU-111 (2.5-80 nM; 24-48 hours) inhibits Panc-1, AsPC-1 and HPAF-II cells growth in a dose and time-dependent manner (24 hours: IC50s of 25, 35 and 35?nM, respectively; 48 hours: IC50s of 11.8, 15.5, and 25?nM, respectively)[4].
? VERU-111 (5-20 nM; 24 hours) arrests Panc-1 and AsPC-1 cells in G2/M phase in a dose-dependent manner[4].
? VERU-111 (5-20?nM; 24 hours) shows dose-dependent inhibition of pro-Caspase 3 and 9 and activation of Caspase-3 and 9, induces the expression of Bax and Bad, and inhibits the expression of Bcl-2 and Bcl-xl proteins in both AsPC-1 and Panc-1 cells[4].

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

Cell Proliferation Assay[4]

Cell Line: Panc-1, AsPC-1, HPAF-II cells
Concentration: 2.5, 5, 10, 20, 40, 80 nM
Incubation Time: 24, 48 hours
Result: Inhibited the growth of PanCa cells in a dose and time-dependent manner. The IC50 of VERU-111 was 25, 35 and 35?nM in Panc-1, AsPC-1 and HPAF-II, respectively after 24?h treatment, while 48?h post-treatment it was 11.8, 15.5, and 25?nM.

Apoptosis Analysis[4]

Cell Line: Panc-1, AsPC-1 cells
Concentration: 5, 10, 20 nM
Incubation Time: 24 hours
Result: Arrested Panc-1 and AsPC-1 cells in G2/M phase in a dose-dependent manner.

Western Blot Analysis[4]

Cell Line: AsPC-1 and Panc-1 cells
Concentration: 5, 10, 20 nM
Incubation Time: 24 hours
Result: Dose-dependent inhibition of pro-Caspase 3 and 9 and activation of Caspase-3 and 9 in both AsPC-1 and Panc-1 cells. Induces the expression of Bax and Bad and inhibited the expression of Bcl-2 and Bcl-xl proteins.
體內(nèi)研究
(In Vivo)

VERU-111 (50?μg/mouse; intra-tumorally; 3 times per week for 3?weeks) effectively inhibits tumor growth as compared to vehicle-treated group. None of the mouse showed any apparent toxicity as constant increase of body weight in VERU-111 treated mice[4].

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

Animal Model: Six-week-old female athymic nude mice (bearing AsPC-1 cells)
Dosage: 50?μg/mouse
Administration: Intra-tumorally; 3 times per week for 3?weeks
Result: Effectively inhibited tumor growth.
Clinical Trial
分子量

377.39

Formula

C21H19N3O4

CAS 號(hào)
性狀

固體

顏色

Light yellow to yellow

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 20 mg/mL (53.00 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 2.6498 mL 13.2489 mL 26.4978 mL
5 mM 0.5300 mL 2.6498 mL 5.2996 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 (sealed storage, away from moisture and light)。-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)

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

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 mg/mL (5.30 mM); 澄清溶液

    此方案可獲得 ≥ 2 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 20.0 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 mg/mL (5.30 mM); 懸濁液; 超聲助溶

    此方案可獲得 2 mg/mL的均勻懸濁液,懸濁液可用于口服和腹腔注射。

    1 mL 工作液為例,取 100 μL 20.0 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

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

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(gòu)。 ,Tween 80,均可在 MCE 網(wǎng)站選購(gòu)。
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)。

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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(guó)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: 99.00%

參考文獻(xiàn)

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 (sealed storage, away from moisture and light)。-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。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6498 mL 13.2489 mL 26.4978 mL 66.2445 mL
5 mM 0.5300 mL 2.6498 mL 5.2996 mL 13.2489 mL
10 mM 0.2650 mL 1.3249 mL 2.6498 mL 6.6244 mL
15 mM 0.1767 mL 0.8833 mL 1.7665 mL 4.4163 mL
20 mM 0.1325 mL 0.6624 mL 1.3249 mL 3.3122 mL
25 mM 0.1060 mL 0.5300 mL 1.0599 mL 2.6498 mL
30 mM 0.0883 mL 0.4416 mL 0.8833 mL 2.2081 mL
40 mM 0.0662 mL 0.3312 mL 0.6624 mL 1.6561 mL
50 mM 0.0530 mL 0.2650 mL 0.5300 mL 1.3249 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.

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產(chǎn)品名稱:
Sabizabulin
目錄號(hào):
HY-120599
需求量: