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  2. MAPK/ERK Pathway Apoptosis
  3. MEK Apoptosis
  4. GDC-0623

GDC-0623  (Synonyms: RG 7421; MEK inhibitor 1)

目錄號: HY-15610 純度: 99.15%
COA 產(chǎn)品使用指南

GDC-0623 (RG 7421) 是一種有效的，ATP 競爭性的 MEK1 抑制劑，Ki值為 0.13 nM，對 HCT116 細(xì)胞中 KRAS (G13D)的 EC50 值為 42 nM，而對 A375 細(xì)胞中 BRAFV600E的 EC50 值為 7 nM。

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GDC-0623 Chemical Structure

GDC-0623 Chemical Structure

CAS No. : 1168091-68-6

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1405
In-stock
1 mg ￥666
In-stock
2 mg ￥950
In-stock
5 mg ￥1400
In-stock
10 mg ￥2248
In-stock
25 mg ￥3259
In-stock
50 mg ￥4400
In-stock
100 mg 現(xiàn)貨 詢價(jià)
200 mg   詢價(jià)  
500 mg   詢價(jià)  

* Please select Quantity before adding items.

查看 MEK 亞型特異性產(chǎn)品:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAFV600E, EC50=7 nM).

IC50 & Target[1]

MEK1

0.13 nM (Ki, +ATP)

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
A-375 EC50
0.004 μM
Compound: G-868, ADS110526, G-049868, GDC-0623
Antiproliferative activity against human A375 cells assessed as inhibition of cell proliferation after 72 hrs
Antiproliferative activity against human A375 cells assessed as inhibition of cell proliferation after 72 hrs
[PMID: 25193232]
HCT-116 EC50
0.051 μM
Compound: G-868, ADS110526, G-049868, GDC-0623
Antiproliferative activity against human HCT116 cells assessed as inhibition of cell proliferation after 72 hrs
Antiproliferative activity against human HCT116 cells assessed as inhibition of cell proliferation after 72 hrs
[PMID: 25193232]
體外研究
(In Vitro)

GDC-0623 (RG 7421) and G-573 are able to prevent MEK phosphorylation by CRAF in vitro, and able to block MEK phosphorylation by BRAF(V600E)[1]. GDC-0623 (RG 7421) is potent, ATP-uncompetitive inhibitors of MEK1 but shows distinct shifts in cellular activity compared with the other two inhibitors, only 6-fold half-maximum effective concentration (EC50) decreases[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

GDC-0623 (RG 7421) (40 mg/kg, p.o.) shows percent tumour growth inhibition (%TGI) in MiaPaCa-2 xenograft model. GDC-0623 (RG 7421) and G-573 show superior antitumour activity compared to GDC-0623 (RG 7421) in all three KRAS models[1].

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

456.21

Formula

C16H14FIN4O3
CAS 號
性狀

固體

顏色

Light yellow to gray

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 50 mg/mL (109.60 mM; 超聲助溶; 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)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.1920 mL 10.9599 mL 21.9197 mL
5 mM 0.4384 mL 2.1920 mL 4.3839 mL
查看完整儲備液配制表

* 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。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時(shí)，請?jiān)?年內(nèi)使用， -20°C儲存時(shí)，請?jiān)?年內(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

動物實(shí)驗(yàn)：

請根據(jù)您的 實(shí)驗(yàn)動物和給藥方式 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，澄清的儲備液可以根據(jù)儲存條件，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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.48 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

    請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.48 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。
動物溶解方案計(jì)算器
請輸入動物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動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。
動物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，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: 99.15%

參考文獻(xiàn)
Cell Assay
[1]

Flag-MEK1 mutants, S212P and S212A, are generated using the QuickChange site directed mutagenesis kit. Mammalian expression vectors for N-terminal Flag tagged MEK-1 are expressed in HCT116 cells. 1.8×106 HCT116 cells are plated in 10 cm plate and transfected on the following day with 17 μg of expression constructs using lipofectamine 2000. After 48 hours cells are treated with inhibitors for the indicated times, harvested and lysed in 100 μL cell extraction buffer. Cell lysates from each sample are analyzed by SDS-PAGE. Membranes are incubated with phospho-MEK S221, phospho-ERK1/2 and MEK1 primary antibodies and immunoreactive proteins are analyzed by SuperSignal West Pico Chemiluminescent Substrate.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Colo205 xenografts are established by inoculating 5×106 cells resuspended in Hank's Balanced Salt Solution (HBSS) subcutaneously (s.c.) in the rear right flank of 6-8 week old female nude (nu/nu) mice. NCI-H2122 xenografts are established by inoculating 1×107 cells resuspended in Hank's Balanced Salt Solution (HBSS) plus matrigel (growth factor reduced) s.c. in the rear right flank of 6-8 week old female nu/nu mice. Both A375 and MiaPaca-2 xenografts are initiated by transplanting 1 mm3 tumor fragments from their respective passaged tumors s.c. into the flank of athymic nu/nu mice. When tumors reached appr 200 mm3, mice are randomized and treated with daily (QD) oral gavage (PO) with either vehicle [methylcellulose 0.1% tween 80 0.1% (MCT)], GDC-0973 (at 10 mg/kg), GDC-0623 (RG 7421) (40 mg/kg), or G-573 (100 mg/kg). All doses of MEK inhibitors represented maximal tolerated doses (MTDs), resulting in no more than 15-20% body weight loss. Tumor volumes are determined using digital calipers using the formula (L×W×W)/2. Tumor growth inhibition (%TGI) iscalculated as the percentage of the area under the fitted curve (AUC) for the respective dose group per day in relation to the vehicle. Animal weights are recorded twice per week and mice are removed from study if body weights dropped ≥20%. Partial responses (PRs) are defined as any tumor demonstrating a ≥ 50% decrease in tumor volume, whereas complete responses (CRs) are defined as any tumor demonstrating 100% reduction in tumor volume at any point during the study.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻(xiàn)

完整儲備液配制表

* 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。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時(shí)，請?jiān)?年內(nèi)使用， -20°C儲存時(shí)，請?jiān)?年內(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 2.1920 mL 10.9599 mL 21.9197 mL 54.7993 mL
5 mM 0.4384 mL 2.1920 mL 4.3839 mL 10.9599 mL
10 mM 0.2192 mL 1.0960 mL 2.1920 mL 5.4799 mL
15 mM 0.1461 mL 0.7307 mL 1.4613 mL 3.6533 mL
20 mM 0.1096 mL 0.5480 mL 1.0960 mL 2.7400 mL
25 mM 0.0877 mL 0.4384 mL 0.8768 mL 2.1920 mL
30 mM 0.0731 mL 0.3653 mL 0.7307 mL 1.8266 mL
40 mM 0.0548 mL 0.2740 mL 0.5480 mL 1.3700 mL
50 mM 0.0438 mL 0.2192 mL 0.4384 mL 1.0960 mL
60 mM 0.0365 mL 0.1827 mL 0.3653 mL 0.9133 mL
80 mM 0.0274 mL 0.1370 mL 0.2740 mL 0.6850 mL
100 mM 0.0219 mL 0.1096 mL 0.2192 mL 0.5480 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：
GDC-0623
目錄號：
HY-15610
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