2. MAPK/ERK Pathway
  3. MEK
  4. Tunlametinib

Tunlametinib  (Synonyms: HL-085)

製品番号: HY-132844 純度: 99.53%
COA 取扱説明書 Technical Support

Tunlametinib is a highly selective, orally active MEK1/2 inhibitor (IC50=1.9 nM, MEK1). Tunlametinib blocks the RAS-RAF-MEK-ERK signaling pathway, arrests tumor cell cycle and promotes apoptosis. Tunlametinib potently inhibits the proliferation of RAS/RAF mutant cancer cells (such as BRAF V600E, KRAS G12C mutant cells). Tunlametinib shows synergistic anti-tumor effects with BRAF/KRASG12C/SHP2 inhibitors, Docetaxel (HY-B0011). Tunlametinib can be used to study targeted therapy for RAS/RAF mutation-driven malignancies (such as melanoma, colorectal cancer, and non-small cell lung cancer).

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Tunlametinib

Tunlametinib 構造式

CAS 番号 : 1801756-06-8

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 211 在庫あり
Solution
10 mM * 1 mL in DMSO USD 211 在庫あり
Solid
5 mg $195 在庫あり
10 mg $304 在庫あり
25 mg $495 在庫あり
50 mg $690 在庫あり
100 mg $970 在庫あり
250 mg $1460 在庫あり
500 mg $2100 在庫あり
1 g $2950 在庫あり
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Tunlametinib 関連抗体

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MEK 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
MEK1 MEK2 MEK5 MEK MAP2K4/MEK4 MAP2K7/MEK7

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製品説明

Tunlametinib is a highly selective, orally active MEK1/2 inhibitor (IC50=1.9 nM, MEK1). Tunlametinib blocks the RAS-RAF-MEK-ERK signaling pathway, arrests tumor cell cycle and promotes apoptosis. Tunlametinib potently inhibits the proliferation of RAS/RAF mutant cancer cells (such as BRAF V600E, KRAS G12C mutant cells). Tunlametinib shows synergistic anti-tumor effects with BRAF/KRASG12C/SHP2 inhibitors, Docetaxel (HY-B0011). Tunlametinib can be used to study targeted therapy for RAS/RAF mutation-driven malignancies (such as melanoma, colorectal cancer, and non-small cell lung cancer)[1][2].

IC50 & Target

MEK1

 

MEK2

 

体外実験

Tunlametinib inhibits the cell viability of BRAF/KRAS mutant cell lines: A375, Colo-829, HL-60 melanoma cells, COLO 205, HT-29 colon cancer cells, Calu-6, A549 lung cancer cells, with IC50 of 0.86 nM, 3.46 nM, 0.67 nM, 0.94 nM, 10.07 nM, 59.89 nM, respectively. Tunlametinib has no significant effect on RAS/RAF wild-type cells (H1975, MRC-5)[1].
Tunlametinib (1-9 nM; 48 h) dose-dependently increases the proportion of A375 cells in the G0/G1 phase and induces cell cycle arrest[1].
Tunlametinib (10-90 nM or 1-9 nM; 48 h) dose-dependently induces apoptosis in COLO 205 cells (10-90 nM), without significant induction effect on A375 cells (1-9 nM)[1].
Tunlametinib (0.1-100 nM; 48 h) dose-dependently reduces the level of phosphorylated ERK (p-ERK) in A375 cells with an IC50 of approximately 1.16 nM. Tunlametinib completely inhibits ERK phosphorylation at a concentration of 100 nM[1].

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

Tunlametinib 関連抗体

Cell Cycle Analysis[1]

Cell Line: A375 (BRAF V600E mutant melanoma)
Concentration: 1 nM, 3 nM, 9 nM
Incubation Time: 48 h
Result: Dose-dependently increased the number of G0/G1 phase cells (from 50% to 70% of total population), indicating cell cycle arrest.

Apoptosis Analysis[1]

Cell Line: A375 (BRAF V600E mutant melanoma) and COLO 205 (BRAF-mutated colon cancer cells)
Concentration: 1 nM, 3 nM, 9 nM for A375 treatment; 10 nM, 30 nM, 90 nM for COLO 205 treatment
Incubation Time: 48 h
Result: Resulted the proportion of apoptosis cells within normal limits, suggesting no significant apoptosis-inducing effect on A375 cells.
Resulted the proportion of apoptosis of 35.1%, 38.4% and 46.6% after treated with 10, 30 and 90 nM, respectively.
体内実験

Tunlametinib (1, 3, 6 mg/kg; oral; once daily; 21 days) dose-dependently inhibits tumor growth in A375 (BRAF V600E mutant melanoma), COLO 205 (BRAF V600E mutant colon cancer), Calu-6 (KRAS Q61K mutant lung cancer) tumor-bearing models in female BALB/c nude mice, NU/NU or Nod-Scid mice, with superior inhibition effect to AZD6244 (HY-50706) (25 mg/kg; BID; 21 days)[1].
Tunlametinib (3, 9 mg/kg; oral; once daily; 21 days) inhibits tumor growth in H1975 (BRAF/KRAS wild-type lung cancer) tumor-bearing model in female BALB/c nude mice[1].
Tunlametinib (1 mg/kg, oral; once daily; 30 days) inhibits tumor growth in BRAF-mutated colorectal cancer patient-derived xenograft (PDX) models (CR0004, CR0029, CR2179, CR6289) without causing significant changes in body weight[1].
Tunlametinib (0.25 mg/kg, 1-10 days; 0.125 mg/kg, 11-21 days; oral, once daily) combined with SHP099 (HY-100388) (I: 50 mg/kg, 1-10 days; II: 25 mg/kg, 10-21 days; oral; once every 2 days), synergistically inhibits tumor growth in the H358 (KRASG12C mutant lung cancer) tumor-bearing model[1].
Tunlametinib (1 mg/kg; oral; once daily; 21 days) combined with AMG 510 (HY-114277) (3 mg/kg; oral; once daily; 21 days), synergistically inhibits tumor growth in KRASG12C mutant tumor-bearing models[1].
Tunlametinib (1 mg/kg; oral; once daily; 10 days) combined with Vemurafenib (HY-12057) (25 mg/kg; oral; twice daily; 10 days), synergistically inhibits tumor growth in A375 (BRAF mutant melanoma) tumor-bearing models[1].
Tunlametinib (0.5 mg/kg; oral; twice daily or 3.5 mg/kg, twice weekly; for 4 weeks) combined with Docetaxel (HY-B0011) (I: 10 mg/kg in weeks 1-2, II: 7.5 mg/kg in week 3, III: 5 mg/kg in week 4; intravenous injection; once a week), synergistically inhibits tumor growth in Calu-6, H358, H441, and A549 (all RAS mutant lung cancer) tumor-bearing models[1].

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

Animal Model: Female BALB/c nude mice (5-8 weeks old) with A375, HT-29, Calu-6 cell-derived xenograft (CDX) model, or CRC atient-derived xenograft (PDX)[1]
Dosage: 1, 3, 6 mg/kg for CDX model; 1 mg/kg (PO) for PDX model
Administration: Oral administration, once daily, 21 days
Result: Significantly inhibited tumor growth in a dose-dependent manner, with better inhibitory effect than that of AZD6244 (25 mg/kg, po, QD).
臨床実験
分子量

491.25

分子式

C16H12F2IN3O3S
CAS 番号
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=CC2=C(C(F)=C1NC3=CC=C(C=C3F)I)N=CS2)NOCCO
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 : 100 mg/mL (203.56 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 2.0356 mL 10.1781 mL 20.3562 mL
5 mM 0.4071 mL 2.0356 mL 4.0712 mL
10 mM 0.2036 mL 1.0178 mL 2.0356 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)

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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

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体積 （開始）

V1

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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: ≥ 5 mg/mL (10.18 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (10.18 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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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: 99.53%

COA (250 KB) HNMR (125 KB) LCMS (104 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 2.0356 mL 10.1781 mL 20.3562 mL 50.8906 mL
5 mM 0.4071 mL 2.0356 mL 4.0712 mL 10.1781 mL
10 mM 0.2036 mL 1.0178 mL 2.0356 mL 5.0891 mL
15 mM 0.1357 mL 0.6785 mL 1.3571 mL 3.3927 mL
20 mM 0.1018 mL 0.5089 mL 1.0178 mL 2.5445 mL
25 mM 0.0814 mL 0.4071 mL 0.8142 mL 2.0356 mL
30 mM 0.0679 mL 0.3393 mL 0.6785 mL 1.6964 mL
40 mM 0.0509 mL 0.2545 mL 0.5089 mL 1.2723 mL
50 mM 0.0407 mL 0.2036 mL 0.4071 mL 1.0178 mL
60 mM 0.0339 mL 0.1696 mL 0.3393 mL 0.8482 mL
80 mM 0.0254 mL 0.1272 mL 0.2545 mL 0.6361 mL
100 mM 0.0204 mL 0.1018 mL 0.2036 mL 0.5089 mL
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Tunlametinib Related Classifications

  • Molarity Calculator

  • Dilution Calculator

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

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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
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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.

Keywords:

Tunlametinib1801756-06-8HL-085HL085HL 085MEKMitogen-activated protein kinase kinaseMAPKKMAP2Ktyrosine kinaseantineoplasticInhibitorinhibitorinhibit

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