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  2. MAPK/ERK Pathway Stem Cell/Wnt Apoptosis
  3. ERK Apoptosis
  4. DEL-22379

DEL-22379 是一種 ERK 二聚化抑制劑。DEL-22379 易與 ERK2 結(jié)合，Kd 為低微摩爾水平，即使在低納摩爾濃度下也可檢測到 EL-22379 與 ERK2 結(jié)合。DEL-22379 抑制 ERK2 二聚化，IC50 約為 0.5 μM。

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DEL-22379 Chemical Structure

DEL-22379 Chemical Structure

CAS No. : 181223-80-3

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10 mM * 1 mL in DMSO ￥825
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5 mg ￥750
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10 mg ￥1300
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50 mg ￥3950
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MCE 顧客使用本產(chǎn)品發(fā)表的 2 篇科研文獻

查看 ERK 亞型特異性產(chǎn)品:

  • 生物活性

  • 實驗參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

DEL-22379 is an ERK dimerization Inhibitor. DEL-22379 readily binds to ERK2 with a Kd estimated in the low micromolar range, though binding is detectable even at low nanomolar concentrations. ERK2 dimerization is progressively inhibited with an IC50 of ~0.5 μM.

IC50 & Target[1]

ERK2

0.5 μM (IC50)

體外研究
(In Vitro)

DEL-22379 is an ERK dimerization inhibitor. DEL-22379 abolishes EGF-induced co-immunoprecipitation of ectopic ERK2 molecules tagged with hemagglutinin (HA) or FLAG epitopes, with an estimated half-maximal inhibitory concentration (IC50) of ~0.5 μM. DEL-22379 inhibits growth of tumor cells harboring RAS-ERK pathway oncogenes. The biological effects of DEL-22379 are investigated on tumor cells in culture. The cytostatic effects of DEL-22379 are compared to those of the MEK inhibitor PD-0325901 and the ERK kinase inhibitor SCH-772984, as reflected by their half-maximal growth inhibitory concentrations (GI50). Cell lines harboring mutant BRAF are the most sensitive to the three compounds. In comparison, wild-type (WT) cell lines for BRAF and RAS are the most resistant, and RAS mutant cells exhibit a range of sensitivities. In cells showing different oncogenic genotypes, distinct sensitivity to DEL-22379 can not be attributed to variations on its effects on dimerization, because DEL-22379 displays similar dimerization- and cytoplasmic signaling-inhibitory dose responses (IC50 of 150-400 nM) regardless of the genotype[1].

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

To test DEL-22379 antitumor effects, some of the aforementioned cell lines are xenografted into nude mice, and tumor growth is monitored after intra-peritoneal administration of DEL-22379 at 15 mg/kg. At such a dose, inhibition of ERK dimerization is evident in liver extracts and in xenografted tumors. DEL-22379 markedly inhibits tumor progression for A375 cells (BRAF mutant)[1].

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

444.53

Formula

C26H28N4O3
CAS 號
性狀

固體

顏色

Yellow to orange

運輸條件

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)
細胞實驗： 

DMSO 中的溶解度 : 100 mg/mL (224.96 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 2.2496 mL 11.2478 mL 22.4957 mL
5 mM 0.4499 mL 2.2496 mL 4.4991 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，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

動物實驗：

請根據(jù)您的 實驗動物和給藥方式 選擇適當?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：
——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；
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 (5.62 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。
動物溶解方案計算器
請輸入動物實驗的基本信息：

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
由于實驗過程有損耗，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。
動物實驗體內(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
參考文獻
Cell Assay
[1]

HEK293T cells are plated at a density of 1,000-2,000 cells/well and treated with DEL-22379 (0.2-1 μ M) for 48 hr, Alamar Blue is added, and the colorimetric change is measured at 570 and 600 nm. GI50 is estimated by nonlinear regression using GraphPad5 Prism Software. Apoptosis is analyzed by evaluating caspase 3 activity, either by western blotting or using the Caspase-Glo 3/7 luminogenic assay[1].

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

Mice[1]
Cancer cells are xenografted in female, athymic nu/nu mice of 8 weeks of age. 3×106 cells are injected subcutaneously in the lateral flank and allowed to develop for 10-15 days before treatment with DEL-22379 at 15 mg/kg every 12 hr for 2 weeks. patient-derived xenografts (PDXs) are performed using patient-derived colorectal cancer cells harboring BRAFV600E from non-necrotic areas of primary adenocarcinomas from patients that undergo surgical resection. Cells are grafted in both flanks or in the cecum of NOD-SCID mice. DEL-22379 is administered by intra-peritoneal injection at a concentration of 15 mg/kg every 12 hr for 30 days[1].

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

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，請在2年內(nèi)使用， -20°C儲存時，請在1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 2.2496 mL 11.2478 mL 22.4957 mL 56.2392 mL
5 mM 0.4499 mL 2.2496 mL 4.4991 mL 11.2478 mL
10 mM 0.2250 mL 1.1248 mL 2.2496 mL 5.6239 mL
15 mM 0.1500 mL 0.7499 mL 1.4997 mL 3.7493 mL
20 mM 0.1125 mL 0.5624 mL 1.1248 mL 2.8120 mL
25 mM 0.0900 mL 0.4499 mL 0.8998 mL 2.2496 mL
30 mM 0.0750 mL 0.3749 mL 0.7499 mL 1.8746 mL
40 mM 0.0562 mL 0.2812 mL 0.5624 mL 1.4060 mL
50 mM 0.0450 mL 0.2250 mL 0.4499 mL 1.1248 mL
60 mM 0.0375 mL 0.1875 mL 0.3749 mL 0.9373 mL
80 mM 0.0281 mL 0.1406 mL 0.2812 mL 0.7030 mL
100 mM 0.0225 mL 0.1125 mL 0.2250 mL 0.5624 mL
Help & FAQs
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    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：
DEL-22379
目錄號：
HY-18932
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