2. Cell Cycle/DNA Damage
  3. Microphthalmia Associated Transcription Factor (MITF)
  4. TT-012

TT-012 is a MITF inhibitor with a human MITF IC50 of 13.1 nM and a human MITF Kd value of 15.5 nM. TT-012 reduces mRNA levels of MITF downstream genes linked to melanosome biogenesis, cell survival, and proliferation, and upregulates cell cycle-inhibiting genes. TT-012 can be used for the research of melanoma[1][2][3].

For research use only. We do not sell to patients.

TT-012

TT-012 Chemical Structure

CAS No. : 1164471-33-3

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Based on 2 publication(s) in Google Scholar

TT-012 Related Antibodies

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Description

TT-012 is a MITF inhibitor with a human MITF IC50 of 13.1 nM and a human MITF Kd value of 15.5 nM. TT-012 reduces mRNA levels of MITF downstream genes linked to melanosome biogenesis, cell survival, and proliferation, and upregulates cell cycle-inhibiting genes. TT-012 can be used for the research of melanoma[1][2][3].

In Vitro

TT-012 inhibits the growth and metastasis of MITF-high melanoma cells by disrupting MITF dimer formation and DNA-binding ability[1].
TT-012 potently and specifically disrupts the dimerization of the human MITF bHLH-LZ domain in a cell-free AlphaScreen assay with an IC50 of 13.1 nM[2].
TT-012 specifically binds the MBP-fused human MITF bHLH-LZ domain in a cell-free SPR assay with a Kd of 15.5 nM[2].
TT-012 (5 μM; 8 h) systematically inhibits the MITF-mediated transcriptional network in B16F10 mouse melanoma cells, down-regulating 33 MITF target genes by more than 2-fold and selectively targeting MITF over other MiT/TFE family members[2].
TT-012 (72 h) potently inhibits the growth of high-MITF B16F10 mouse melanoma cells with an IC50 of 499 nM, with reduced activity in cells overexpressing MITF or the stable MITFΔ3 mutant, and shows selective activity against high-MITF melanoma cell lines[2].
TT-012 (10 μM; 1 h) increases the proportion of monomeric endogenous MITF in B16F10 mouse melanoma cells[3].
TT-012 (1 h) dose-dependently reduces endogenous MITF dimer formation in B16F10 mouse melanoma cells[3].
TT-012 (1.56-50 μM; 8 h) dose-dependently reduces mRNA levels of MITF target genes Tyr and Trpm1 in B16F10 mouse melanoma cells, with IC50 values less than 3.12 μM[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TT-012 Related Antibodies

Real Time qPCR[2]

Cell Line: B16F10 mouse melanoma cells
Concentration: 1.56 μM; 3.12 μM; 6.25 μM; 12.5 μM; 25 μM; 50 μM
Incubation Time: 8 h
Result: Dose-dependently reduced the mRNA levels of MITF target genes Tyr and Trpm1, with IC50 values less than 3.12 μM.
In Vivo

TT-012 (2-5 mg/kg; i.v.; once every 2 days; 5 total doses) potently inhibits subcutaneous B16F10 melanoma growth in C57BL/6 mice[2].
TT-012 (2-5 mg/kg; i.v.; once every 2 days; 18 days) significantly inhibits B16F10 melanoma pulmonary metastasis in C57BL/6 mice[2].
TT-012 (10 mg/kg; i.v.; three times weekly) inhibits tumor growth in a high-MITF melanoma patient-derived xenograft model, with no activity in a low-MITF PDX model[2].
TT-012 (2-5 mg/kg; i.v.; once every 2 days) reduces subcutaneous melanoma tumor weight in female C57BL/6 mice, with tolerable toxicity to liver and immune cells[3].
TT-012 (2-5 mg/kg; i.v.; once every 2 days; 18 days) reduces melanoma pulmonary metastatic burden by ~99% at 5 mg/kg and significantly reduces metastatic niches at 2 mg/kg in female C57BL/6 mice[3].
TT-012 (10 mg/kg; i.v.; three times weekly) inhibits tumor growth in high-MITF melanoma patient-derived xenografts in NPSG mice[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 (female, 6-8 weeks old, subcutaneous implantation of B16F10 melanoma cells)[2]
Dosage: 2 mg/kg; 5 mg/kg
Administration: i.v.; once every 2 days; 5 total doses
Result: Potently suppressed tumor growth (P < 0.0001).
Reduced average tumor weight by 79.7% (2 mg/kg) compared to vehicle controls.
Reduced average tumor weight by 93.9% (5 mg/kg) compared to vehicle controls.
Showed no significant difference in body weight compared to vehicle-treated mice.
Caused no significant changes in frequencies of major lymphoid and myeloid subsets across tested tissues.
Caused no significant changes in GPT or ALP levels, indicating no apparent liver damage.
Animal Model: C57BL/6 (female, 6-8 weeks old, intravenous tail vein injection of B16F10 melanoma cells)[2]
Dosage: 2 mg/kg; 5 mg/kg
Administration: i.v.; once every 2 days; 18 days
Result: Caused a significant decrease in lung metastatic burden (P < 0.0001) at 2 mg/kg compared to vehicle controls.
Reduced metastatic burden by ~99% at 5 mg/kg compared to vehicle controls (P < 0.0001).
Animal Model: NPSG (implanted with patient-derived melanoma tissue)[2]
Dosage: 10 mg/kg
Administration: i.v.; three times weekly
Result: Attenuated xenograft tumor growth in the high-MITF PDX-case 7 model.
Showed no effect in the low-MITF PDX-case 6 model.
Animal Model: C57BL/6 (female, 6-8 weeks old)[3]
Dosage: 2 mg/kg; 5 mg/kg
Administration: i.v.; once every 2 days
Result: Suppressed tumor growth (P < 0.0001).
Reduced average tumor weight by 79.7% (2 mg/kg) compared to vehicle-treated mice.
Reduced average tumor weight by 93.9% (5 mg/kg) compared to vehicle-treated mice.
Showed no significant changes in body weight, frequencies of major lymphoid/myeloid immune cell subsets, or liver function markers (GPT, ALP).
Animal Model: C57BL/6 (female, 6-8 weeks old)[3]
Dosage: 2 mg/kg; 5 mg/kg
Administration: i.v.; once every 2 days; 18 days
Result: Reduced lung metastatic burden significantly (P < 0.0001) at 2 mg/kg compared to vehicle controls.
Reduced metastatic burden by ~99% (P < 0.0001) at 5 mg/kg compared to vehicle controls.
Animal Model: NPSG (implanted with patient-derived melanoma tissue)[3]
Dosage: 10 mg/kg
Administration: i.v.; three times weekly
Result: Attenuated xenograft tumor growth of PDX-case 7 (high MITF).
Reduced tumor volumes significantly compared to vehicle controls by day 12.
Molecular Weight

349.34

Formula

C19H15N3O4
CAS No.
Appearance

Solid

Color

Light yellow to brown

SMILES

O=C(/C=C/C1=CC=CO1)NC2=CC=CC(NC(/C=C/C3=CC=CO3)=O)=N2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (286.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (7.16 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: 2.5 mg/mL (7.16 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8625 mL 14.3127 mL 28.6254 mL 71.5635 mL
5 mM 0.5725 mL 2.8625 mL 5.7251 mL 14.3127 mL
10 mM 0.2863 mL 1.4313 mL 2.8625 mL 7.1564 mL
15 mM 0.1908 mL 0.9542 mL 1.9084 mL 4.7709 mL
20 mM 0.1431 mL 0.7156 mL 1.4313 mL 3.5782 mL
25 mM 0.1145 mL 0.5725 mL 1.1450 mL 2.8625 mL
30 mM 0.0954 mL 0.4771 mL 0.9542 mL 2.3855 mL
40 mM 0.0716 mL 0.3578 mL 0.7156 mL 1.7891 mL
50 mM 0.0573 mL 0.2863 mL 0.5725 mL 1.4313 mL
60 mM 0.0477 mL 0.2385 mL 0.4771 mL 1.1927 mL
80 mM 0.0358 mL 0.1789 mL 0.3578 mL 0.8945 mL
100 mM 0.0286 mL 0.1431 mL 0.2863 mL 0.7156 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TT-0121164471-33-3TT012TT 012Microphthalmia Associated Transcription Factor (MITF)Microphthalmia Associated Transcription Factormelanosome biogenesismelanomapatient-derived xenograft modelB16F10 mouse melanoma cellsMiT/TFE family membersTrpm1TyrMITFC57BL/6 miceNPSG miceInhibitorinhibitorinhibit

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