| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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CU-T12-9 (CU T12-9; CU-T129) is a novel and potent TLR1/2 (Toll-like receptor) agonist with potential immunemodulatory and antitumor effects. Toll-like receptor (TLR) agonists activate both the innate and the adaptive immune systems. Thus, TLR agonists have been exploited as potent vaccine adjuvants and antitumor agents. CU-T12-9 activates TLR1/2 with an EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay. CU-T12-9 signals through nuclear factor κB (NF-κB) and invokes an elevation of the downstream effectors tumor necrosis factor-α (TNF-α), interleukin-10 (IL-10), and inducible nitric oxide synthase (iNOS).
| ln Vitro |
CU-T12-9 directly targets TLR1/2 to activate downstream signaling. By binding to TLR1 and TLR2, CU-T12-9 stimulates the development of the TLR1/2 heterodimer complex, thereby activating downstream signaling [1]. CU-T12-9 promotes downstream signaling, such as secretory embryonic alkaline phosphatase (SEAP), NO and TNF-α, via triggering NF-κB activation, thereby activating the TLR1/2 pathway [1]. CU-T12-9 (0.39-100 μM; 24 hours) does not generate toxicity up to 100 μM in HEK-Blue hTLR2 and Raw 264.7 cells [1]. CU-T12-9 upregulates the mRNA levels of TLR1, TLR2, TNF, IL-10, and iNOS. CU-T12-9 (0.1-10 μM) stimulates TLR1 mRNA and iNOS mRNA 24 hours after treatment of Raw 264.7 cells. CU-T12-9 (0.1-10 μM) activates TLR2 and IL-10 mRNA after 2 hours of stimulation of Raw 264.7 cells. CU-T12-9 (0.1-10 μM) activates TNF mRNA after 8 hours of treatment in Raw 264.7 cells [1].
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| Cell Assay |
Cytotoxicity assay[1]
Cell Types: HEK-Blue hTLR2 and Raw 264.7 Macrophage Tested Concentrations: 0.39, 0.78, 1.56, 3.125, 6.25, 12.5, 25, 50 and 100 μM Incubation Duration: 24 hrs (hours) Experimental Results: No toxicity observed Up to 100 μM. RT-PCR[1] Cell Types: Original 264.7 Cell Tested Concentrations: 0.1, 1, 10 μM Incubation Duration: TLR1 and iNOS mRNA assayed for 24 hrs (hours) TLR2 and IL-10 mRNA assayed for 2 hrs (hours) TNF mRNA assayed for 8 hrs (hours) Experimental Results: Triggered TLR1 mRNA and iNOS mRNA were dose-dependent at 24 hrs (hours). Dose-dependent activation of TLR2 mRNA and IL-10 mRNA at 2 hrs (hours). Dose-dependent activation of TNF mRNA was shown at 8 hrs (hours). |
| References |
[1]. Cheng K, et al. Specific activation of the TLR1-TLR2 heterodimer by small-molecule agonists. Sci Adv. 2015;1(3). pii: e1400139.
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| Molecular Formula |
C17H13F3N4O2
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|---|---|
| Molecular Weight |
362.31
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| Exact Mass |
362.0991
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| CAS # |
1821387-73-8
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| SMILES |
CNC1=CC=C([N+]([O-])=O)C=C1N1C=NC(C2=CC=C(C(F)(F)F)C=C2)=C1
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| Synonyms |
CUT129 CU T12 9 CU-T12-9
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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 : ~250 mg/mL (~690.02 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.74 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 | 2.7601 mL | 13.8003 mL | 27.6007 mL | |
| 5 mM | 0.5520 mL | 2.7601 mL | 5.5201 mL | |
| 10 mM | 0.2760 mL | 1.3800 mL | 2.7601 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.
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