BTX-7312
Based on 1 Customer Validation
BTX-7312 is a potent SOS1 molecular glue degrader. BTX-7312 forms a ternary complex by linking the target protein SOS1 with the E3 ubiquitin ligase cereblon, inducing ubiquitination and degradation of SOS1, thereby blocking the RAS/MAPK and PI3K/AKT signaling pathways and consequently inhibiting cell proliferation. BTX-7312 can be used for research on KRAS-driven cancers.
For research use only. We do not sell to patients.
- Purity : 98.35%
- Formula: C45H52ClF4N9O6
- Molecular Weight:926.40
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MIA PaCa-2 | DC50 |
0.5 nM
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Degradation of SOS1 in human MIA PaCa-2 cells incubated 24 hrs by immunoblotting.
Degradation of SOS1 in human MIA PaCa-2 cells incubated 24 hrs by immunoblotting.
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38224565 |
| LoVo | DC50 |
3.9 nM
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Degradation of SOS1 in human LoVo cells incubated 24 hrs by immunoblotting.
Degradation of SOS1 in human LoVo cells incubated 24 hrs by immunoblotting.
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38224565 |
| MIA PaCa-2 | IC50 |
1.1 nM
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Inhibition of pAKT (S473) in 3D human MIA PaCa-2 cells incubated 24 hrs by immunoblotting.
Inhibition of pAKT (S473) in 3D human MIA PaCa-2 cells incubated 24 hrs by immunoblotting.
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38224565 |
| LoVo | IC50 |
26.3 nM
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Inhibition of pERK in 3D human LoVo cells incubated 24 hrs by immunoblotting.
Inhibition of pERK in 3D human LoVo cells incubated 24 hrs by immunoblotting.
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38224565 |
| A549 | IC50 |
44.2 nM
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Inhibition of pS6 (S235/S236) in 3D human A549 cells incubated 24 hrs by immunoblotting.
Inhibition of pS6 (S235/S236) in 3D human A549 cells incubated 24 hrs by immunoblotting.
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38224565 |
| EBC-1 | IC50 |
38.7 nM
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Antiproliferative activity against human EBC-1 cells after 3 days by CellTiter-Glo assay.
Antiproliferative activity against human EBC-1 cells after 3 days by CellTiter-Glo assay.
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38224565 |
| EBC-1 | IC50 |
9.4 nM
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Antiproliferative activity against human EBC-1 cells in 3D culture after 5-6 days by CellTiter-Glo assay.
Antiproliferative activity against human EBC-1 cells in 3D culture after 5-6 days by CellTiter-Glo assay.
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38224565 |
| NCI-H358 | IC50 |
> 10000 nM
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Antiproliferative activity against human NCI-H358 cells after 3 days by CellTiter-Glo assay with IC50 >10,000 nM.
Antiproliferative activity against human NCI-H358 cells after 3 days by CellTiter-Glo assay with IC50 >10,000 nM.
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38224565 |
| NCI-H358 | IC50 |
1.8 nM
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Antiproliferative activity against human NCI-H358 cells in 3D culture after 5-6 days by CellTiter-Glo assay.
Antiproliferative activity against human NCI-H358 cells in 3D culture after 5-6 days by CellTiter-Glo assay.
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38224565 |
| MIA PaCa-2 | IC50 |
> 10000 nM
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Antiproliferative activity against human MIA PaCa-2 cells after 3 days by CellTiter-Glo assay with IC50 >10,000 nM.
Antiproliferative activity against human MIA PaCa-2 cells after 3 days by CellTiter-Glo assay with IC50 >10,000 nM.
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38224565 |
| MIA PaCa-2 | IC50 |
> 2500 nM
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Antiproliferative activity against SOS1 knockout human MIA PaCa-2 cells in 3D culture with IC50 >2,500 nM.
Antiproliferative activity against SOS1 knockout human MIA PaCa-2 cells in 3D culture with IC50 >2,500 nM.
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38224565 |
| MIA PaCa-2 | DC50 |
1.6 nM
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Antiproliferative activity against SOS2 knockout human MIA PaCa-2 cells in 3D culture.
Antiproliferative activity against SOS2 knockout human MIA PaCa-2 cells in 3D culture.
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38224565 |
| HEK293 | IC50 |
5 μM
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Antiproliferative activity against human HEK293 cells with IC50 >5 μM.
Antiproliferative activity against human HEK293 cells with IC50 >5 μM.
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38224565 |
In Vitro
BTX-7312 synergizes with Sotorasib (HY-114277), Trametinib (HY-10999), Afatinib (HY-10261), and MRTX1133 (HY-134813) in 3D proliferation assays across KRAS-mutant cell lines[1].
BTX-7312 (0.3 nM-2 μM; 24 h) dose-dependently degrades SOS1 protein in MIA PaCa-2 and LoVo cells, with DC50 values of 0.5 nM and 3.9 nM, respectively, and does not affect the expression of proteins such as SOS2[1].
BTX-7312 (50-200 nM; 1-6 h) induces time-dependent degradation of SOS1 protein in MIA PaCa-2 and LoVo cells[1].
BTX-7312 (50-200 nM; 6 h) degrades wild-type SOS1 in H358 parental cells and in cells with knockout and knock-in of SOS1 mutants, but does not degrade H905V or N879A/H905V mutant SOS1[1].
BTX-7312 (0.8-500 nM; 6-24 h) reduces the levels of downstream signaling proteins pERK and pS6 (S235/S236) in MIA PaCa-2, LoVo, and A549 cells[1].
BTX-7312 has a slight inhibitory effect on cell viability in HEK293 and NHLF cells (IC50 > 5 µM)[1].
BTX-7312 (0.3 nM-2 μM; 24 h) does not induce the degradation of proteins such as EGFR, SHP2, GRB2, and KRAS in MIA PaCa-2 cells[1].
BTX-7312 (0.2-5 µM; 24 h) does not affect CK1α protein expression in MIA PaCa-2 and LoVo cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MIA PaCa-2 and LoVo
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Concentration:0.3, 0.9, 2.7, 8.2, 24, 74, 222, 670, 2000 nM
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Incubation Time:24 h
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Result:Degraded SOS1 protein in a dose-dependent manner, with DC50 values of 0.5 nM and 3.9 nM, respectively.
- BrdU Incorporation Assay
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- MTT Cell Proliferation Assay
Chemical Information
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Appearance Solid
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Molecular Weight 926.40
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Formula C45H52ClF4N9O6
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Color White to off-white
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SMILES
FC(F)(F)C1=CC([C@@H](C)NC2=NC(Cl)=NC3=C2CN(C(C4(OC)CCN(C(CCCCN5CCC(C6=CC(CN(C7CCC(NC7=O)=O)C8=O)=C8C=C6F)CC5)=O)CC4)=O)C3)=CC(N)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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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 (107.94 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. 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. 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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.70 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.70 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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 (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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. 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 | 1.0794 mL | 5.3972 mL | 10.7945 mL | 26.9862 mL |
| 5 mM | 0.2159 mL | 1.0794 mL | 2.1589 mL | 5.3972 mL | |
| 10 mM | 0.1079 mL | 0.5397 mL | 1.0794 mL | 2.6986 mL | |
| 15 mM | 0.0720 mL | 0.3598 mL | 0.7196 mL | 1.7991 mL | |
| 20 mM | 0.0540 mL | 0.2699 mL | 0.5397 mL | 1.3493 mL | |
| 25 mM | 0.0432 mL | 0.2159 mL | 0.4318 mL | 1.0794 mL | |
| 30 mM | 0.0360 mL | 0.1799 mL | 0.3598 mL | 0.8995 mL | |
| 40 mM | 0.0270 mL | 0.1349 mL | 0.2699 mL | 0.6747 mL | |
| 50 mM | 0.0216 mL | 0.1079 mL | 0.2159 mL | 0.5397 mL | |
| 60 mM | 0.0180 mL | 0.0900 mL | 0.1799 mL | 0.4498 mL | |
| 80 mM | 0.0135 mL | 0.0675 mL | 0.1349 mL | 0.3373 mL | |
| 100 mM | 0.0108 mL | 0.0540 mL | 0.1079 mL | 0.2699 mL |
BTX-7312 Related Classifications
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