| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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Purity: ≥98%
LUT014 is a novel, potent and topical B-Raf inhibitor that is a first-in-class, proprietary small molecule that enables patients to receive EGFR (Epidermal Growth Factor Receptor) Inhibitors without being interrupted by typical cutaneous side effects. Lutris-Pharma is working on LUT014 at the moment. LUT014 reduces the dermal toxicities associated with EGFR Inhibitors, thereby reducing the acneiform lesions associated with such therapy by taking advantage of the paradoxical effect of B-Raf Inhibitors.
| Targets |
B-Raf (IC50 = 11.7 nM); BRAF (IC50 = 14 nM); CRAF (IC50 = 23 nM)
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| References | |
| Additional Infomation |
BRAF Inhibitor LUT014 is a topically bioavailable small molecule inhibitor of serine/threonine-protein kinase B-raf (BRAF) protein with potential chemoprotective activity. Upon topical administration, BRAF inhibitor LUT014 targets and binds BRAF and, through the paradoxical effect of BRAF inhibition, induces mitogen-activated protein kinase (MAPK) signaling, which leads to the proliferation and migration of healthy human keratinocytes. This decreases dermal toxicities associated with epidermal growth factor (EGFR) inhibitor therapy. BRAF, a member of the raf family of serine/threonine protein kinases, plays a role in the regulation of MAPK/extracellular signal-regulated kinase (ERK) signaling pathways.
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| Molecular Formula |
C27H19F3N8O
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|---|---|
| Molecular Weight |
528.487974405289
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| Exact Mass |
528.16
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| Elemental Analysis |
C, 61.36; H, 3.62; F, 10.78; N, 21.20; O, 3.03
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| CAS # |
2274819-46-2
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| Related CAS # |
2274819-46-2
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| PubChem CID |
138319775
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
6.2
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
39
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| Complexity |
808
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
FZPYULHBUBXPIG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H19F3N8O/c1-15-7-8-19-18(9-11-32-24(19)37-16-4-2-5-17(12-16)39-27(28,29)30)21(15)38-25-20(6-3-10-31-25)22-23-26(35-13-33-22)36-14-34-23/h2-14H,1H3,(H,31,38)(H,32,37)(H,33,34,35,36)
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| Chemical Name |
6-methyl-5-N-[3-(7H-purin-6-yl)pyridin-2-yl]-1-N-[3-(trifluoromethoxy)phenyl]isoquinoline-1,5-diamine
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| Synonyms |
LUT 014; LUT014; LUT-014
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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: ~50 mg/mL (~94.6 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.94 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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8922 mL | 9.4609 mL | 18.9218 mL | |
| 5 mM | 0.3784 mL | 1.8922 mL | 3.7844 mL | |
| 10 mM | 0.1892 mL | 0.9461 mL | 1.8922 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04759664 | Recruiting | Drug: LUT014 Gel (Dose 1) Drug: LUT014 Gel (Dose 2) |
EGFRI Induced Acneiform Lesions |
Lutris Pharma Ltd. | April 12, 2021 | Phase 2 |
| NCT04261387 | Completed | Drug: LUT014 Gel Drug: Placebo for LUT014 Gel |
Radiation Dermatitis | Lutris Pharma Ltd. | January 30, 2021 | Phase 1 Phase 2 |
| NCT03876106 | Completed | Drug: LUT014 | EGFR Inhibitor Induced Acneiform Lesions |
Lutris Pharma Ltd. | August 21, 2019 | Phase 1 |
Products are for research use only; We do not sell to patients
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