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  1. Stem Cell/Wnt Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling Autophagy Apoptosis
  2. JAK Autophagy Apoptosis
  3. Icaritin

Icaritin  (Synonyms: 脫水淫羊藿素; Anhydroicaritin)

目錄號(hào): HY-N0678 純度: 99.35%
COA 產(chǎn)品使用指南 技術(shù)支持

Icaritin (Anhydroicaritin) 是淫羊藿中的異戊二烯類(lèi)黃酮衍生物,有效抑制 K562 細(xì)胞 (IC50 為 8 μM) 和原代 CML 細(xì)胞 (對(duì) CML-CP 的 IC50 值為 13.4 μM,對(duì) CML-BC 的 IC50 值為 18 μM) 的增殖。Icaritin 可以調(diào)節(jié) MAPK/ERK/JNKJAK2/STAT3/AKT 信號(hào)傳導(dǎo),并具有增強(qiáng)成骨的作用。

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Icaritin Chemical Structure

Icaritin Chemical Structure

CAS No. : 118525-40-9

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10 mM * 1 mL in DMSO ¥660
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1 mg ¥300
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5 mg ¥600
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10 mg ¥1100
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25 mg ¥1815
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50 mg ¥2541
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100 mg ¥3557
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Customer Review

Other Forms of Icaritin:

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

查看 JAK 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Icaritin (Anhydroicaritin) is a prenylflavonoid derivative from Epimedium brevicornuMaxim. and potently inhibits proliferation of K562 cells (IC50 of 8 μM) and primary CML cells (IC50 of 13.4 μM for CML-CP and 18 μM for CML-BC). Icaritin can regulate MAPK/ERK/JNK and JAK2/STAT3 /AKT signalings, also enhances osteogenesis[1][2][3.

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
> 100 μM
Compound: 1
Cytotoxicity against human A549 cells assessed as cell viability by MTT assay
Cytotoxicity against human A549 cells assessed as cell viability by MTT assay
[PMID: 26079090]
Hep 3B2 IC50
0.9 μM
Compound: ICT; 1
Antiproliferative activity against human Hep3B cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human Hep3B cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 36745506]
HepG2 IC50
> 10 μM
Compound: ICT; 1
Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 36745506]
MCF7 IC50
7 μM
Compound: 1
Cytotoxicity against human MCF7 cells assessed as cell viability by MTT assay
Cytotoxicity against human MCF7 cells assessed as cell viability by MTT assay
[PMID: 26079090]
MDA-MB-435S IC50
24.9 μM
Compound: 1
Cytotoxicity against human MDA-MB-435S cells assessed as cell viability by MTT assay
Cytotoxicity against human MDA-MB-435S cells assessed as cell viability by MTT assay
[PMID: 26079090]
NCI/ADR-RES IC50
52.09 μM
Compound: 3
Cytotoxicity against human MCF7/ADR cells after 72 hrs by MTT assay
Cytotoxicity against human MCF7/ADR cells after 72 hrs by MTT assay
[PMID: 19523827]
RPMI-8226 IC50
20.78 μM
Compound: Icaritin
Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay
[PMID: 34644502]
SMMC-7721 IC50
> 10 μM
Compound: ICT; 1
Antiproliferative activity against human SMMC-7721 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human SMMC-7721 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 36745506]
Vero IC50
21.6 μM
Compound: 1
Cytotoxicity against African green monkey Vero cells assessed as cell viability by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as cell viability by MTT assay
[PMID: 26079090]
體外研究
(In Vitro)

Icaritin (4-64 μM;48 小時(shí);K562、伊馬替尼耐藥細(xì)胞和原代 CML 細(xì)胞) 處理可抑制 K562、伊馬替尼耐藥細(xì)胞和原代 CML 細(xì)胞的增殖[1]
Icaritin (0-64 μM;48 小時(shí);K562 和原代細(xì)胞) 處理以濃度依賴(lài)性方式誘導(dǎo) K562 或原代細(xì)胞凋亡[1]。
Icaritin (32 μM;K562 細(xì)胞) 處理增加了 K562 細(xì)胞中亞 G1 期的細(xì)胞群[1]。
Icaritin (0-64 μM;48 小時(shí);K562 細(xì)胞) 處理抑制 MAPK/ERK/JNK 下游信號(hào)并減少 Jak2/Stat3/Akt 的表達(dá)。淫羊藿素處理還顯著抑制 K562 中 Bcl-2 蛋白表達(dá)和上調(diào) Bax 蛋白表達(dá),并呈劑量依賴(lài)性,伴隨著 caspase-3 或 caspase-9 的切割激活,以及 Apaf-1 的下調(diào)表達(dá)[1]。

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

Cell Proliferation Assay[1]

Cell Line: K562, imatinib-resistant cells and primary CML cells
Concentration: 4 μM, 8 μM, 16 μM, 32 μM and 64 μM
Incubation Time: 48 hours
Result: Inhibited cell proliferation.

Apoptosis Analysis[1]

Cell Line: K562 or primary cells
Concentration: 0 μM, 4 μM, 8 μM, 16 μM, 32 μM and 64 μM
Incubation Time: 48 hours
Result: Induced K562 or primary cells apoptosis.

Cell Cycle Analysis[1]

Cell Line: K562 cells
Concentration: 32 μM
Incubation Time:
Result: Cell population in the sub-G1 phase was increased.

Western Blot Analysis[1]

Cell Line: K562 cells
Concentration: 0 μM, 4 μM, 8 μM, 16 μM, 32 μM and 64 μM
Incubation Time: 48 hours
Result: Inhibited MAPK/ERK/JNK downstream signaling and diminishes Jak2/Stat3/Akt expression.
體內(nèi)研究
(In Vivo)

Icaritin (4-8 mg/kg;腹腔注射;每日一次;連續(xù)10周;雌性NOD-SCID裸鼠) 處理可延長(zhǎng)接種 K562 細(xì)胞的 NOD-SCID 裸鼠的壽命,而不抑制小鼠白血病模型的骨髓[1]。

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

Animal Model: Female NOD-SCID nude mice (6-8 weeks old) with K562 cells[1]
Dosage: 4 mg/kg and 8 mg/kg
Administration: Intraperitoneal injection; daily; for 10 weeks
Result: Could prolong lifespan of NOD-SCID nude mice inoculated with K562 cells without suppression of bone marrow.
Clinical Trial
分子量

368.38

Formula

C21H20O6

CAS 號(hào)
性狀

固體

顏色

Light yellow to yellow

中文名稱(chēng)

去水淫羊藿黃素;三七淫羊藿素

結(jié)構(gòu)分類(lèi)
初始來(lái)源
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 1 year
-20°C 6 months
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 15.62 mg/mL (42.40 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(kāi)封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.7146 mL 13.5729 mL 27.1459 mL
5 mM 0.5429 mL 2.7146 mL 5.4292 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, 1 year; -20°C, 6 months。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過(guò)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: ≥ 1.56 mg/mL (4.23 mM); 澄清溶液

    此方案可獲得 ≥ 1.56 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 15.6 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。

以下溶解方案,請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配,在短期內(nèi)盡快用完。 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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過(guò)加熱和/或超聲的方式助溶。

  • 方案 一

    請(qǐng)依序添加每種溶劑: 50% PEG300    50% Saline

    Solubility: 1.51 mg/mL (4.10 mM); 懸濁液; 超聲助溶

  • 方案 二

    請(qǐng)依序添加每種溶劑: 15% Cremophor EL    85% Saline

    Solubility: 10 mg/mL (27.15 mM); 懸濁液; 超聲助溶

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(guò)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(guò) 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)。
您所需的儲(chǔ)備液濃度超過(guò)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(guò)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: 99.35%

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, 1 year; -20°C, 6 months。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(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 2.7146 mL 13.5729 mL 27.1459 mL 67.8647 mL
5 mM 0.5429 mL 2.7146 mL 5.4292 mL 13.5729 mL
10 mM 0.2715 mL 1.3573 mL 2.7146 mL 6.7865 mL
15 mM 0.1810 mL 0.9049 mL 1.8097 mL 4.5243 mL
20 mM 0.1357 mL 0.6786 mL 1.3573 mL 3.3932 mL
25 mM 0.1086 mL 0.5429 mL 1.0858 mL 2.7146 mL
30 mM 0.0905 mL 0.4524 mL 0.9049 mL 2.2622 mL
40 mM 0.0679 mL 0.3393 mL 0.6786 mL 1.6966 mL
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產(chǎn)品名稱(chēng):
Icaritin
目錄號(hào):
HY-N0678
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