Art. -Nr.: HY-132844

Tunlametinib

(Synonyms: HL-085)

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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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Reinheit: 99.53%
CAS. Nr.: 1801756-06-8
Formel: C₁₆H₁₂F₂IN₃O₃S
Molecular Weight:491.25

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Tunlametinib Chemical Structure

CAS. Nr.: 1801756-06-8

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

MEK1

MEK2

Alle MEK Isoform-spezifische Produkte anzeigen :

In Vitro

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.

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.

In Vivo

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 (KRAS^G12C 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 KRAS^G12C 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).

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1801756-06-8
Appearance Solid
Molecular Weight 491.25
Formel C₁₆H₁₂F₂IN₃O₃S
Color Off-white to light yellow
SMILES

O=C(C1=CC2=C(C(F)=C1NC3=CC=C(C=C3F)I)N=CS2)NOCCO
Synonyms

HL-085
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Liu Y, et al. Preclinical characterization of tunlametinib, a novel, potent, and selective MEK inhibitor. Front Pharmacol. 2023 Sep 21;14:1271268. [Content Brief]

[2]. Sari MHM, et al. Editorial: Advances in molecular and pharmacological mechanisms of novel targeted therapies for melanoma. Front Oncol. 2024 Apr 4;14:1403778. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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Alle MEK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Tunlametinib Related Classifications

HY-132844 Related Classifications