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50mg |
MRT67307 HCl (MRT 67307; MRT-67307), the hydrochloride salt of MRT-67307, is a multi-kinase inhibitor with potential antitumor activity. It inhibits TBK1, IKKε , MARK1-4 and NUAK1 with IC50 values of 19, 160, 27-52 and 230nM, respectively.
ln Vitro |
MRT67307 did not inhibit IKKα or IKKβ even at 10 μM, however it did inhibit IKKϵ and TBK1 with IC50 values of 160 and 19 nM when 0.1 mM ATP was detected in vitro [1]. In bone marrow-derived macrophages (BMDM), MRT67307 (2 μM) inhibits the phosphorylation of IRF3. Poly(I:C) activation of JNK and p38 MAPK is not inhibited by MRT67307 (2 μM) [1]. IFNβ production in macrophages is inhibited by MRT67307 (1 nM–10 μM) [1]. To get phospho-ATG13 down to acceptable levels, MRT67307 (10 μM) is adequate [2]. In mouse embryonic fibroblasts (MEFs), MRT67307 (10 μM) inhibits autophagy [2]. In 293T cells, MRT67307 (5 µM; 4 hours) completely eliminates TBK1/IKKε-induced CYLD phosphorylation [3].
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Cell Assay |
Western Blot Analysis[3]
Cell Types: 293T Cell Tested Concentrations: 5 µM Incubation Duration: 4 hrs (hours) Experimental Results: Elimination of TBK1/IKKε-induced CYLD phosphorylation. |
References |
[1]. Clark K, et al. Novel cross-talk within the IKK family controls innate immunity. Biochem J. 2011 Feb 15;434(1):93-104.
[2]. Petherick KJ, et al. Pharmacological inhibition of ULK1 kinase blocks mammalian target of rapamycin (mTOR)-dependent autophagy. J Biol Chem. 2015 May 1;290(18):11376-83. [3]. Zhu Z, et al. Inhibition of KRAS-driven tumorigenicity by interruption of an autocrine cytokine circuit. 26.37Cancer Discov. 2014 Apr;4(4):452-65. |
Molecular Formula |
C₂₆H₃₇CLN₆O₂
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Molecular Weight |
501.06
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CAS # |
2095432-39-4
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Related CAS # |
MRT67307;1190378-57-4;MRT67307 dihydrochloride;1781882-89-0
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SMILES |
N(C1=NC(NC2C=CC=C(CN3CCOCC3)C=2)=NC=C1C1CC1)CCCNC(C1CCC1)=O.Cl
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Synonyms |
MRT67307 HCl MRT-67307 HCl
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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 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.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.9958 mL | 9.9788 mL | 19.9577 mL | |
5 mM | 0.3992 mL | 1.9958 mL | 3.9915 mL | |
10 mM | 0.1996 mL | 0.9979 mL | 1.9958 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.