| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| References | |
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| Additional Infomation |
Luvometinib is a small molecule drug. The INN prefix "-tinib" in its name indicates that Luvometinib is a tyrosine kinase inhibitor. Luvometinib is currently being investigated in the clinical trial NCT07004075 (FCN-159 monotherapy versus investigator-selected chemotherapy in pediatric patients with BRAF gene mutations low-grade gliomas). The monoisotope molecular weight of Luvometinib is 665.04 Da. Luvometinib is an orally bioavailable inhibitor of mitogen-activated protein kinase kinases (MAP2K, MAPK/ERK kinases, or MEK) 1 and 2 with potential antitumor activity. After administration, Luvometinib selectively binds to and inhibits the activity of MEK1 and MEK2, thereby preventing the activation of MEK1/2-dependent effector proteins and transcription factors, which may lead to the suppression of growth factor-mediated cell signaling and tumor cell proliferation. MEK1/2 are bispecific threonine/tyrosine kinases that play a crucial role in the activation of the RAS/RAF/MEK/ERK signaling pathway, which regulates cell growth. Mutations in the BRAF, KRAS, and NRAS genes often lead to abnormal activation of this pathway in various tumor cells.
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| Molecular Formula |
C26H22F2IN5O4S
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|---|---|
| Molecular Weight |
665.45
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| Exact Mass |
665.041
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| CAS # |
2739690-43-6
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| Related CAS # |
Luvometinib-d
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| PubChem CID |
135210935
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| Appearance |
Light yellow to yellow solid
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| tPSA |
120
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
39
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| Complexity |
1270
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN1C2=C(C(=C(C1=O)F)NC3=C(C=C(C=C3)I)F)C(=O)N(N=C2C4=CC(=CC=C4)NS(=O)(=O)C5CC5)C6CC6
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| InChi Key |
RJFDJJABNSVLRB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H22F2IN5O4S/c1-33-24-20(23(21(28)26(33)36)30-19-10-5-14(29)12-18(19)27)25(35)34(16-6-7-16)31-22(24)13-3-2-4-15(11-13)32-39(37,38)17-8-9-17/h2-5,10-12,16-17,30,32H,6-9H2,1H3
|
| Chemical Name |
N-[3-[6-cyclopropyl-3-fluoro-4-(2-fluoro-4-iodoanilino)-1-methyl-2,5-dioxopyrido[2,3-d]pyridazin-8-yl]phenyl]cyclopropanesulfonamide
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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 (~150.3 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.76 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.76 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well.  (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5027 mL | 7.5137 mL | 15.0274 mL | |
| 5 mM | 0.3005 mL | 1.5027 mL | 3.0055 mL | |
| 10 mM | 0.1503 mL | 0.7514 mL | 1.5027 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/NCT07562581
Conditions:Non-small Cell Lung Caner|KRAS-mutated|Metastasis|Previous TreamtedLink: https://clinicaltrials.gov/ct2/show/NCT07431060
Conditions:Langerhans Cell Histiocytosis (LCH)Link: https://clinicaltrials.gov/ct2/show/NCT07371182
Conditions:Langerhans Cell Histiocytosis (LCH)
Title:Phase II Study of FCN-159 in NF2 Nerve Sheath Tumors
Status:Recruiting
updateDate:2025-07-29
Ctid:NCT06553365
Link: https://clinicaltrials.gov/ct2/show/NCT06553365
Conditions:Nerve Sheath TumorLink: https://clinicaltrials.gov/ct2/show/NCT07024394
Conditions:Neurofibromatosis 1|Plexiform Neurofibroma|NF1Link: https://clinicaltrials.gov/ct2/show/NCT07004075
Conditions:Low-grade Glioma|Pediatric Low-grade Gliomas|pLGG With BRAF AlterationLink: https://clinicaltrials.gov/ct2/show/NCT06913725
Conditions:Brain Arteriovenous MalformationsLink: https://clinicaltrials.gov/ct2/show/NCT05997602
Conditions:Langerhans Cell Histiocytosis|LCHLink: https://clinicaltrials.gov/ct2/show/NCT04954001
Conditions:Neurofibromatosis 1|Plexiform Neurofibroma|NF1