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  2. Apoptosis Membrane Transporter/Ion Channel
  3. Apoptosis GLUT
  4. GLUT4-IN-2

GLUT4-IN-2 是一種有效的選擇性 GLUT4 抑制劑，對 GLUT1 和 GLUT4 的 IC50s 分別為 11.4 μM 和 6.8 μM。GLUT4-IN-2 誘導(dǎo)細(xì)胞凋亡 (apoptosis) 和細(xì)胞周期停滯在 G0/G1 期。GLUT4-IN-2 顯示出有效的抗腫瘤活性。

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GLUT4-IN-2 Chemical Structure

GLUT4-IN-2 Chemical Structure

CAS No. : 2454113-83-6

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10 mM * 1 mL in DMSO ￥1650
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25 mg ￥5500
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Customer Review

查看 GLUT 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

GLUT4-IN-2 is a potent and selective GLUT4 inhibitor with IC50s of 11.4 μM and 6.8 μM for GLUT1 and GLUT4, respectively. GLUT4-IN-2 induces cell apoptosis and cell cycle arrest at G0/G1phase. GLUT4-IN-2 shows potent antitumor activity[1].

IC50 & Target[1]

GLUT1

11.4 μM (IC50)

GLUT4

6.8 μM (IC50)

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
CCRF-CEM CC50
1.7 μM
Compound: F18
Cytotoxicity against human CCRF-CEM cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis
Cytotoxicity against human CCRF-CEM cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis
[PMID: 32634629]
HS27 CC50
44 μM
Compound: F18
Cytotoxicity against human HS27 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis
Cytotoxicity against human HS27 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis
[PMID: 32634629]
K562 CC50
91.9 μM
Compound: F18
Cytotoxicity against human K562 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis
Cytotoxicity against human K562 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis
[PMID: 32634629]
KCL-22 CC50
15.3 μM
Compound: F18
Cytotoxicity against human KCL-22 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis
Cytotoxicity against human KCL-22 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis
[PMID: 32634629]
MDA-MB-231 CC50
45.1 μM
Compound: F18
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis
[PMID: 32634629]
體外研究
(In Vitro)

GLUT4-IN-2 (compound F18) induces cell apoptosis and ell cycle arrest at G0/G1phase in CME cells[1].
GLUT4-IN-2 (10 μM; 6 h) decreases the expression of mTOR and CDK2, but increases the expression of GRP78, and cleaved caspase 3 proteins [1].

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

Cell Viability Assay[1]

Cell Line: CME, K562, KCL-22, MB-231, HS-27 cells
Concentration: 1-100 μM
Incubation Time: 48 h
Result: Showed potent cytotoxicity with cytotoxic concentration 50% (CC50) of 1.7, 91.9, 15.3, 45.1, 44.0 μM for CME, K562, KCL-22, MB-231, HS-27 cells, respectively.

Apoptosis Analysis[1]

Cell Line: CEM cells
Concentration: 1.7 μM
Incubation Time: 24 h
Result: Induced cell apoptosis with the percentage of apoptotic cells in the late and early apoptosis region was 55.87% and 1.38%, respectively.

Cell Cycle Analysis[1]

Cell Line: CEM cells
Concentration: 10, 25, 50 μM
Incubation Time: 72 h
Result: Induced cell cycle arrest at G0/G1phase in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: CEM cells
Concentration: 10 μM
Incubation Time: 6 h
Result: Decreased the phosphorylation of mTOR and CDK2 proteins and increased the expression of GRP78, and cleaved caspase 3.

Cell Cytotoxicity Assay[1]

Cell Line: CEM cells
Concentration: 2.5-100 μM
Incubation Time: 48 h
Result: Showed cytotoxicity with the IC50s of 1.7, 187.2 μM for CEM, WBCs cells respectively.
體內(nèi)研究
(In Vivo)

GLUT4-IN-2 (50 mg/kg; i.p. on day 1–5, 8–12, 15–18) shows antitumor activity in CEM xenograft model[1].

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

Animal Model: 8–10 weeks, SCID mice (CEM xenograft tumor) [1]
Dosage: 50 mg/kg
Administration: I.p.; administered on day 1-5, 8-12, 15-18
Result: Showed potent antitumor activity in vivo.
分子量

385.42

Formula

C17H11N3O4S2
CAS 號(hào)
性狀

固體

顏色

Off-white to light 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 (259.46 mM; 超聲助溶 (<80°C); 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.5946 mL 12.9729 mL 25.9457 mL
5 mM 0.5189 mL 2.5946 mL 5.1891 mL
查看完整儲(chǔ)備液配制表

* 請根據(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?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請?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

    請依序添加每種溶劑： 10% DMSO    90% Corn Oil

    Solubility: 2.5 mg/mL (6.49 mM); 澄清溶液; 超聲助溶

    此方案可獲得 2.5 mg/mL的澄清溶液，此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。

    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玉米油中，混合均勻。

動(dòng)物溶解方案計(jì)算器
請輸入動(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

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)測溶解度，以下方案僅供參考，如有需要，請與 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，請謹(jǐn)慎選擇該方案。
請確保第一步儲(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
參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請根據(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?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請?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 2.5946 mL 12.9729 mL 25.9457 mL 64.8643 mL
5 mM 0.5189 mL 2.5946 mL 5.1891 mL 12.9729 mL
10 mM 0.2595 mL 1.2973 mL 2.5946 mL 6.4864 mL
15 mM 0.1730 mL 0.8649 mL 1.7297 mL 4.3243 mL
20 mM 0.1297 mL 0.6486 mL 1.2973 mL 3.2432 mL
25 mM 0.1038 mL 0.5189 mL 1.0378 mL 2.5946 mL
30 mM 0.0865 mL 0.4324 mL 0.8649 mL 2.1621 mL
40 mM 0.0649 mL 0.3243 mL 0.6486 mL 1.6216 mL
50 mM 0.0519 mL 0.2595 mL 0.5189 mL 1.2973 mL
60 mM 0.0432 mL 0.2162 mL 0.4324 mL 1.0811 mL
80 mM 0.0324 mL 0.1622 mL 0.3243 mL 0.8108 mL
100 mM 0.0259 mL 0.1297 mL 0.2595 mL 0.6486 mL
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產(chǎn)品名稱：
GLUT4-IN-2
目錄號(hào)：
HY-146980
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