| Size | Price | Stock | Qty |
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| 10mg |
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| Other Sizes |
| Targets |
MEK1 and MEK2 (mitogen-activated protein kinase kinases). Tunlametinib is a highly selective MEK1/2 inhibitor, with a reported IC50 of 1.9 nM for MEK1, demonstrating potent inhibition of the MAPK pathway.
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| ln Vitro |
Tunlametinib inhibits MEK1 with an IC50 of 1.9 nM. It effectively blocks the phosphorylation of ERK, a downstream effector of the MAPK pathway, in tumor cells. It has potent anti-proliferative activity against cancer cells harboring BRAF V600E or KRAS G12C mutations, inducing cell cycle arrest and apoptosis in vitro.
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| ln Vivo |
Tunlametinib is currently in clinical development. In preclinical models, it exhibits potent activity against BRAF- and RAS-mutant tumors. Its selectivity for MEK1/2 reduces off-target toxicities. It has also shown synergistic effects when combined with BRAF, KRAS G12C, or SHP2 inhibitors, as well as with docetaxel.
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| Enzyme Assay |
Cell-free MEK1 activity assays are performed using recombinant human MEK1 enzyme. The enzyme is incubated with a substrate (inactive ERK) and ATP in the presence of increasing concentrations of Tunlametinib. The reaction is terminated, and MEK1 activity is measured by quantifying the phosphorylation of ERK using a luminescence-based detection system. IC50 is calculated.
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| Cell Assay |
BRAF V600E or KRAS G12C mutant cancer cell lines are seeded in 96-well plates and treated with increasing concentrations of Tunlametinib for 72 hours. Cell viability is assessed by the MTT assay or CellTiter-Glo. ERK phosphorylation (p-ERK) and PARP cleavage are measured by Western blot to evaluate pathway inhibition and apoptosis.
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| Animal Protocol |
For in vivo studies, Tunlametinib is administered orally to mice bearing subcutaneous xenografts of BRAF-mutant melanoma or KRAS-mutant NSCLC. Dosing is typically once daily for 2-4 weeks. Tumor volumes are measured with calipers. At study termination, tumors are excised for analysis of p-ERK levels and Ki-67 immunohistochemistry to assess pharmacodynamics.
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| ADME/Pharmacokinetics |
Tunlametinib is an orally bioavailable small-molecule MEK inhibitor. It has a molecular weight of 491.25 g/mol and a molecular formula of C16H12F2IN3O3S. Its physicochemical properties support once-daily oral dosing. Pharmacokinetic parameters (t1/2, Cmax, AUC, F%) have been optimized for robust systemic exposure in preclinical and clinical models.
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| Toxicity/Toxicokinetics |
In preclinical studies, Tunlametinib is generally well-tolerated with a manageable safety profile. Class-related adverse events of MEK inhibitors, such as skin rash and diarrhea, are expected. As an investigational new drug, its safety is being evaluated in Phase 1/2 clinical trials. No significant off-target toxicities have been reported.
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| References | |
| Additional Infomation |
Tunlametinib is an orally bioavailable inhibitor of mitogen-activated protein kinases (MAP2K, MAPK/ERK kinases, or MEK) with potential antitumor activity. After administration, Tunlametinib selectively binds to and inhibits MEK activity, thereby preventing the activation of MEK-dependent effector proteins and transcription factors, which may lead to the suppression of growth factor-mediated cell signaling and tumor cell proliferation. MEK is a threonine/tyrosine kinase that plays a crucial role in the activation of the RAS/RAF/MEK/ERK pathway, which regulates cell growth. Mutations in the BRAF, KRAS, and NRAS genes lead to aberrant activation of this pathway in various tumor cell types.
Other information: Tunlametinib (HL-085, CAS 1801756-06-8) is an investigational drug. It is a highly selective MEK1/2 inhibitor that has been evaluated in clinical trials for the treatment of BRAF V600E mutant melanoma. It is not yet FDA-approved. It is a valuable tool for researching the MAPK pathway in RAS/RAF-driven cancers. |
| Molecular Formula |
C16H12F2IN3O3S
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|---|---|
| Molecular Weight |
491.251061439514
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| Exact Mass |
490.961
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| CAS # |
1801756-06-8
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| PubChem CID |
71621329
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
4
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
26
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| Complexity |
496
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1C2=CC(C(NOCCO)=O)=C(NC3=CC=C(I)C=C3F)C(F)=C2N=C1
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| InChi Key |
UFZJUVFSSINETF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H12F2IN3O3S/c17-10-5-8(19)1-2-11(10)21-14-9(16(24)22-25-4-3-23)6-12-15(13(14)18)20-7-26-12/h1-2,5-7,21,23H,3-4H2,(H,22,24)
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| Chemical Name |
4-fluoro-5-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethoxy)-1,3-benzothiazole-6-carboxamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 100 mg/mL (203.56 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Link: https://clinicaltrials.gov/ct2/show/NCT07507526
Conditions:Gastric AdenocarcinomaLink: https://clinicaltrials.gov/ct2/show/NCT07463677
Conditions:Lung Cancer (NSCLC)Link: https://clinicaltrials.gov/ct2/show/NCT07445022
Conditions:Melanoma Advanced
Title:Phase II Trial of Tunlametinib in Patients With NRAS Mutant Non-melanoma Refractory Solid Tumors
Status:Recruiting
updateDate:2025-09-12
Ctid:NCT07170293
Link: https://clinicaltrials.gov/ct2/show/NCT07170293
Conditions:Solid CancersLink: https://clinicaltrials.gov/ct2/show/NCT06970353
Conditions:Radioactive Iodine-refractory, Differentiated Thyroid Cancer With NRAS Mutation|Advanced PDTC or ATC With NRAS MutationLink: https://clinicaltrials.gov/ct2/show/NCT06008106
Conditions:MelanomaLink: https://clinicaltrials.gov/ct2/show/NCT05900219
Conditions:Non-small-cell Lung CancerLink: https://clinicaltrials.gov/ct2/show/NCT05233332
Conditions:CRCLink: https://clinicaltrials.gov/ct2/show/NCT03973151
Conditions:MelanomaLink: https://clinicaltrials.gov/ct2/show/NCT05217303
Conditions:MelanomaLink: https://clinicaltrials.gov/ct2/show/NCT05331105
Conditions:Neurofibromatosis 1|Plexiform NeurofibromasLink: https://clinicaltrials.gov/ct2/show/NCT05263453
Conditions:MelanomaLink: https://clinicaltrials.gov/ct2/show/NCT03781219
Conditions:Solid TumorLink: https://clinicaltrials.gov/ct2/show/NCT04683354
Conditions:Solid Tumor, AdultLink: https://clinicaltrials.gov/ct2/show/NCT03990077
Conditions:NsclcLink: https://clinicaltrials.gov/ct2/show/NCT03976050
Conditions:Solid Tumor, AdultProducts are for research use only; We do not sell to patients
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