MYC degrader 1 TFA
Based on 1 publication(s) in Google Scholar
MYC degrader 1 TFA is a MYC degrader that recruits Cereblon (CRBN), with a Kd value of 145 nM and oral activity. MYC degrader 1 TFA specifically binds MYC and GSPT1, recruits the CRBN E3 ubiquitin ligase complex, and induces MYC degradation via the ubiquitin-proteasome pathway. MYC degrader 1 TFA downregulates KLHL42 expression, restores pRB1 protein levels, and re-establishes the sensitivity of MYC-overexpressing cancer cells to CDK4/6 inhibitors. MYC degrader 1 TFA combined with Palbociclib (HY-50767) shows significant inhibition of tumor growth. MYC degrader 1 TFA can be used in studies related to bladder cancer, prostate cancer, and breast cancer.
For research use only. We do not sell to patients.
- Purity : 99.36%
- Formula: C34H32ClF6N5O5
- Molecular Weight:740.09
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Storage:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) MYC degrader 1 TFA
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Biological Activity
Description
In Vitro
MYC degrader 1 (compound A80.2HCl) TFA binds to purified MYC protein with a dissociation constant of 145 nM[1].
MYC degrader 1 TFA directly binds to the CRBN protein[1].
MYC degrader 1 TFA promotes the interaction between endogenous CRBN and MYC in T24 bladder cancer cells[1].
MYC degrader 1 TFA mediates MYC degradation in T24 bladder cancer cells in a CRBN-dependent manner[1].
MYC degrader 1 TFA inhibits colony formation of T24, UMUC14 bladder cancer cells, C4-2 prostate cancer cells, and MDA-MB-231 breast cancer cells, and its activity depends on MYC expression[1].
MYC degrader 1 TFA inhibits cell viability, with an IC50 range of 12 nM to 78 nM in T24 and UMUC14 bladder cancer cells, C4-2 prostate cancer cells, and MDA-MB-231 breast cancer cells, and its activity is dependent on MYC expression[1].
MYC degrader 1 TFA enhances the efficacy of CDK4/6 inhibitors (Palbociclib, Abemaciclib (HY-16297A), Ribociclib (HY-15777)) in T24 and UMUC14 bladder cancer cells, reduces the IC50 of Palbociclib, and induces synergistic cytotoxicity[1].
MYC degrader 1 TFA enhances the ability of CDK4/6 inhibitors (Palbociclib, Abemaciclib, Ribociclib) to suppress colony formation of T24 and UMUC14 bladder cancer cells[1].
MYC degrader 1 (2-50 nM) TFA induces proteasomal degradation of MYC, reduces KLHL42 expression, and increases the stability of pRB1 protein in T24 bladder cancer cells, C4-2 prostate cancer cells, and MDA-MB-231 breast cancer cells[1].
MYC degrader 1 (10 nM; 24 h) TFA inhibits the transcriptional activity of MYC and downregulates the target genes of MYC and E2F in T24 bladder cancer cells[1].
MYC degrader 1 (10 nM; 24 h) TFA combined with Palbociclib (HY-50767) (1 μM) shows stronger inhibition of MYC and E2F target genes in T24 bladder cancer cells than either agent alone[1].
MYC degrader 1 TFA overcomes the acquired resistance of cells to CDK4/6 inhibitors by resensitizing T24 bladder cancer cells to Palbociclib[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:T24, C4-2, MDA-MB-231, 22RV1, T47D and UMUC14 cell lines
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Concentration:0, 10, 25, 50, 100, 500 and 1000 nM
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Incubation Time:24 h
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Result:Reduced KLHL42 levels and increased RB1 levels.
In Vivo
MYC degrader 1 (6 mg/kg; p.o.; once daily; study terminated on day 30) TFA enhances the antitumor efficacy of Palbociclib in UMUC14 bladder cancer xenografts[1].
MYC degrader 1 TFA inhibits the growth of T24 bladder cancer xenografts in a MYC-dependent manner and reduces MYC protein levels in tumor tissues[1].
MYC degrader 1 (6 mg/kg; p.o.; once daily; for 7 consecutive days) TFA enhances the antitumor efficacy of Palbociclib in MYC-amplified breast cancer mini-PDX models[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male nude mice were subcutaneously inoculated with T24 cells (1×106 suspended in 100 μL of serum-free DMEM, mixed with Matrigel at a 1:1 ratio) on the right side of the abdomen to induce tumor formation. Subsequent experiments were started when the tumor volume reached 100-150 mm3[1]
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Dosage:6 mg/kg
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Administration:p.o.; daily; harvesting tumors on the 30th day after cancer cell inoculation
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Result:Significantly inhibited T24 xenograft tumor growth.
Produced more profound reduction in tumor volume when combined with palbociclib compared to either single agent.\nProduced more profound reduction in UMUC14 xenograft tumor volume when combined with palbociclib compared to either single agent.
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Animal Model:Male NSG mice[1]
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Dosage:6 mg/kg (in combination with palbociclib)
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Administration:p.o.; daily (in combination with Palbociclib); harvesting tumors on the 30th day after cancer cell inoculation
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Result:Significantly inhibited T24 xenograft tumor growth.
Had little effect on MYC-knockdown xenograft tumors.
Markedly decreased MYC protein levels in treated tumors.
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Animal Model:5-week-old female nu/nu mice[1]
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Dosage:6 mg/kg
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Administration:p.o.; daily; 7 days
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Result:Showed no significant effect on tumor cell growth in MYC-amplified breast cancer mini-PDX models when administered alone.
Markedly enhanced the growth-inhibitory efficacy of palbociclib when combined.
Chemical Information
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Appearance Solid
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Molecular Weight 740.09
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Formula C34H32ClF6N5O5
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Color White to off-white
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SMILES
ClC1=CC(C2=CC(C(F)(F)F)=C(N3CCC(CNCC4=CC(CN(C5C(NC(CC5)=O)=O)C6=O)=C6C=C4)CC3)N=C2)=CC=C1.O=C(O)C(F)(F)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (1)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
BCR::ABL1-Induced Enhancer Reprogramming Uncovers Hypersensitivity of Ph+B-ALL Cells to Enhancer-Targeting Drugs. [Abstract]2026 Mar 1:e17231. PMID: 41764406
Solvent & Solubility
In Vitro:
DMSO : 200 mg/mL (270.24 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (6.76 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (298 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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 (sealed storage, away from moisture and light). 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 | 1.3512 mL | 6.7559 mL | 13.5119 mL | 33.7797 mL |
| 5 mM | 0.2702 mL | 1.3512 mL | 2.7024 mL | 6.7559 mL | |
| 10 mM | 0.1351 mL | 0.6756 mL | 1.3512 mL | 3.3780 mL | |
| 15 mM | 0.0901 mL | 0.4504 mL | 0.9008 mL | 2.2520 mL | |
| 20 mM | 0.0676 mL | 0.3378 mL | 0.6756 mL | 1.6890 mL | |
| 25 mM | 0.0540 mL | 0.2702 mL | 0.5405 mL | 1.3512 mL | |
| 30 mM | 0.0450 mL | 0.2252 mL | 0.4504 mL | 1.1260 mL | |
| 40 mM | 0.0338 mL | 0.1689 mL | 0.3378 mL | 0.8445 mL | |
| 50 mM | 0.0270 mL | 0.1351 mL | 0.2702 mL | 0.6756 mL | |
| 60 mM | 0.0225 mL | 0.1126 mL | 0.2252 mL | 0.5630 mL | |
| 80 mM | 0.0169 mL | 0.0844 mL | 0.1689 mL | 0.4222 mL | |
| 100 mM | 0.0135 mL | 0.0676 mL | 0.1351 mL | 0.3378 mL |
MYC degrader 1 TFA Related Classifications
HY-162318A Related Classifications
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