2. MAPK/ERK Pathway Stem Cell/Wnt Apoptosis
  3. ERK Apoptosis
  4. ASTX029

ASTX029 (Example 1) is a potent dual ERK1/2 inhibitor (IC50: 2.7 nM). ASTX029 has anti-cancer activity.

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ASTX029

ASTX029 構造式

CAS 番号 : 2095719-92-7

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 154 在庫あり
Solution
10 mM * 1 mL in DMSO USD 154 在庫あり
Solid
5 mg $120 在庫あり
10 mg $190 在庫あり
25 mg $300 在庫あり
50 mg $540 在庫あり
100 mg $950 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 7 publication(s) in Google Scholar

ASTX029 関連抗体

Top Publications Citing Use of Products

ERK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
ERK ERK1 ERK2 ERK5 ERK8

  • 生物活性

  • 純度とドキュメンテーション

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製品説明

ASTX029 (Example 1) is a potent dual ERK1/2 inhibitor (IC50: 2.7 nM). ASTX029 has anti-cancer activity[1][2].

IC50 & Target[1]

ERK1

 

ERK2

 

Cellular Effect
Cell Line Type Value Description References
A-375 IC50
3.4 1
Compound: 15
Antiproliferative activity against human A-375 cells assessed as reduction in cell viability after 96 hrs by alamar blue assay
Antiproliferative activity against human A-375 cells assessed as reduction in cell viability after 96 hrs by alamar blue assay
[PMID: 34387469]
A-375 IC50
3.4 1
Compound: 15
Antiproliferative activity against human A-375 cells assessed as reduction in cell viability after 96 hrs by alamar blue assay
Antiproliferative activity against human A-375 cells assessed as reduction in cell viability after 96 hrs by alamar blue assay
[PMID: 34387469]
A-375 IC50
3.4 1
Compound: 15
Antiproliferative activity against human A-375 cells assessed as reduction in cell viability after 96 hrs by alamar blue assay
Antiproliferative activity against human A-375 cells assessed as reduction in cell viability after 96 hrs by alamar blue assay
[PMID: 34387469]
COLO 205 IC50
3.6 1
Compound: 15
Antiproliferative activity against human COLO 205 cells assessed as reduction in cell viability after 96 hrs by alamar blue assay
Antiproliferative activity against human COLO 205 cells assessed as reduction in cell viability after 96 hrs by alamar blue assay
[PMID: 34387469]
COLO 205 IC50
3.6 1
Compound: 15
Antiproliferative activity against human COLO 205 cells assessed as reduction in cell viability after 96 hrs by alamar blue assay
Antiproliferative activity against human COLO 205 cells assessed as reduction in cell viability after 96 hrs by alamar blue assay
[PMID: 34387469]
COLO 205 IC50
3.6 1
Compound: 15
Antiproliferative activity against human COLO 205 cells assessed as reduction in cell viability after 96 hrs by alamar blue assay
Antiproliferative activity against human COLO 205 cells assessed as reduction in cell viability after 96 hrs by alamar blue assay
[PMID: 34387469]
体外実験

ASTX029 (96 h) inhibits the proliferation of human cancer cells with MAPK-activating mutations, with IC50 values of 1.8 to 380 nM[2].
ASTX029 (2 h) inhibits the phosphorylation of RSK in both A375 and HCT116 cells, with IC50 values of 3.3 and 4 nM respectively, and also reduces pERK level[2].
ASTX029 (10 and 100 nM, 0-72 h) induces cell-cycle to arrest in the G1-phase, and induces cell apoptosis in A375 and HCT116 cells[2].

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

ASTX029 関連抗体

Western Blot Analysis[2]

Cell Line: A375 and HCT116 cells
Concentration: 1 nM-100 nM
Incubation Time: 2 h
Result: Decreased pRSK and pERK.

Apoptosis Analysis[2]

Cell Line: A375 and HCT116 cells
Concentration: 0-100 nM
Incubation Time: 0-72 h
Result: Arrested cell in the G1-phase.
Increased cleaved PARP and Bim protein level.
体内実験

ASTX029 (20-75 mg/kg, p.o.) inhibits tumor growth in Colo205 (BRAFV600E-mutant colorectal cancer) tumor-bearing mice[2].
ASTX029 (5 mg/kg, p.o., mice) shows AUC of 1600 ng h/mL, T1/2 of 2.9 h, F (%) of 42%[3].

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

Animal Model: Colo205, A375, Calu-6, HCC44, HCT116 or MA-MEL-28 xenografts tumor-bearing mice[2]
Dosage: 75 mg/kg
Administration: p.o., once daily
Result: Inhibited tumor growth in various tumor models.
臨床実験
分子量

584.04

分子式

C29H31ClFN5O5
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

ClC(C(C1=CC2=C(CN([C@H](C)C(N[C@H](CO)C3=CC(F)=CC(OC)=C3)=O)C2=O)C=C1)=N4)=CN=C4NC5CCOCC5
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 250 mg/mL (428.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7122 mL 8.5611 mL 17.1221 mL
5 mM 0.3424 mL 1.7122 mL 3.4244 mL
10 mM 0.1712 mL 0.8561 mL 1.7122 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

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体積 （終了）

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (3.56 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.08 mg/mL (3.56 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.86%

COA (251 KB) HNMR (294 KB) LCMS (94 KB)

取扱説明書 (2659 KB)
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7122 mL 8.5611 mL 17.1221 mL 42.8053 mL
5 mM 0.3424 mL 1.7122 mL 3.4244 mL 8.5611 mL
10 mM 0.1712 mL 0.8561 mL 1.7122 mL 4.2805 mL
15 mM 0.1141 mL 0.5707 mL 1.1415 mL 2.8537 mL
20 mM 0.0856 mL 0.4281 mL 0.8561 mL 2.1403 mL
25 mM 0.0685 mL 0.3424 mL 0.6849 mL 1.7122 mL
30 mM 0.0571 mL 0.2854 mL 0.5707 mL 1.4268 mL
40 mM 0.0428 mL 0.2140 mL 0.4281 mL 1.0701 mL
50 mM 0.0342 mL 0.1712 mL 0.3424 mL 0.8561 mL
60 mM 0.0285 mL 0.1427 mL 0.2854 mL 0.7134 mL
80 mM 0.0214 mL 0.1070 mL 0.2140 mL 0.5351 mL
100 mM 0.0171 mL 0.0856 mL 0.1712 mL 0.4281 mL
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ASTX029 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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.

Keywords:

ASTX0292095719-92-7ASTX 029ASTX-029ERKApoptosisExtracellular signal regulated kinasesA375HCT116tumoranticancerInhibitorinhibitorinhibit

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製品番号:
HY-126288
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