| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
TT-012 targets the microphthalmia-associated transcription factor (MITF), a key regulator of melanocyte development and melanoma progression. It specifically binds to dynamic MITF and disrupts its dimer formation and DNA binding ability. It inhibits the transcriptional activity of MITF in B16F10 melanoma cells.
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|---|---|
| ln Vitro |
In vitro, TT-012 inhibits the growth of high-MITF melanoma cells. It inhibits MITF-MITF dimerization with an IC50 of 13.1 nM in AlphaScreen assays. It inhibits the transcriptional activity of MITF in B16F10 melanoma cells. It is a powerful research tool for studying transcription factor regulation and melanoma biology.
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| ln Vivo |
In vivo, TT-012 inhibits tumor growth and metastasis with tolerable toxicity to liver and immune cells in animal models. It shows potential for the development of targeted therapies for MITF-driven cancers. It inhibits the growth of high-MITF melanoma cells in xenograft models.
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| Enzyme Assay |
Cell-free assays for TT-012: MITF-MITF dimerization is measured using AlphaScreen assays. The compound is incubated with MITF protein and AlphaScreen beads. Signal is measured and IC50 values are calculated. DNA binding ability of MITF is assessed by electrophoretic mobility shift assays (EMSA) or DNA-binding ELISA.
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| Cell Assay |
Cellular assays for TT-012: B16F10 melanoma cells are cultured and treated with TT-012 at concentrations of 0.1-100 µM for 24-72 hours. MITF transcriptional activity is measured by luciferase reporter assays. Cell proliferation is measured by MTT or colony formation assays. Apoptosis is assessed by Annexin V/PI staining. MITF target gene expression is measured by qPCR.
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| Animal Protocol |
In vivo animal studies for TT-012: xenograft mouse models of melanoma are used. Mice are implanted with high-MITF melanoma cells and treated with TT-012 at doses of 1-10 mg/kg. Tumor growth and metastasis are monitored. Toxicity to liver and immune cells is assessed. MITF activity and downstream signaling are evaluated in tumor tissues.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of TT-012: as a small molecule (molecular weight 349.34), it may have moderate oral bioavailability and tissue distribution. It likely penetrates cells to inhibit MITF dimerization. Metabolism and elimination pathways require further investigation. Detailed PK data are limited.
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| Toxicity/Toxicokinetics |
Toxicity of TT-012: in animal models, TT-012 shows tolerable toxicity to liver and immune cells. However, comprehensive toxicity data are limited. It is for research use only and not approved for clinical use. Standard laboratory safety precautions should be followed.
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| References | |
| Additional Infomation |
TT-012 is a research compound with potential applications in melanoma research and targeted cancer therapy. It is available as a reference standard for pharmacological studies. Its mechanism involves disruption of MITF dimerization and inhibition of MITF transcriptional activity. No clinical trials or FDA approvals have been reported.
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| Molecular Formula |
C19H15N3O4
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|---|---|
| Molecular Weight |
349.34
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| Exact Mass |
349.106
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| CAS # |
1164471-33-3
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| PubChem CID |
2165557
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| Appearance |
Light yellow to brown solid powder
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| Density |
1.385±0.06 g/cm3(Predicted)
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| Boiling Point |
654.9±55.0 °C(Predicted)
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| LogP |
2.2
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
26
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| Complexity |
503
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O1C=CC=C1/C=C/C(NC1C=CC=C(N=1)NC(/C=C/C1=CC=CO1)=O)=O
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| InChi Key |
YUFJMFXVUUMVCA-GFULKKFKSA-N
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| InChi Code |
InChI=1S/C19H15N3O4/c23-18(10-8-14-4-2-12-25-14)21-16-6-1-7-17(20-16)22-19(24)11-9-15-5-3-13-26-15/h1-13H,(H2,20,21,22,23,24)/b10-8+,11-9+
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| Chemical Name |
(E)-3-(furan-2-yl)-N-[6-[[(E)-3-(furan-2-yl)prop-2-enoyl]amino]pyridin-2-yl]prop-2-enamide
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.8625 mL | 14.3127 mL | 28.6254 mL | |
| 5 mM | 0.5725 mL | 2.8625 mL | 5.7251 mL | |
| 10 mM | 0.2863 mL | 1.4313 mL | 2.8625 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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