VUBI1
Based on 1 Customer Validation
VUBI1 (SOS1 activator 1) is a benzimidazole derivative and SOS1 activator with a Kd of 44 nM. VUBI1 can significantly activate RAS-GTP and regulate the phosphorylation of ERK. VUBI1 also can serve as a target ligand for synthesizing PROTACs, such as PROTAC SOS1 degrader-1 (HY-145737), to induce SOS1 degradation. VUBI1 can be used in the study of cancer.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
The VUBI1 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
- Purity : 98.21%
- CAS No.: 2245237-53-8
- 화학식: C26H32ClFN6
- 분자량:483.02
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보관:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
In Vitro
VUBI1 (Compound 64) (0.3-30 µM; 10 min) increases RAS-GTP levels and biphasically modulates ERK1/2 phosphorylation in HeLa cells (inducing peak levels at low concentrations and suppressing at high concentrations)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa cells
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Concentration:0.3, 1, 3, 10 and 30 µM
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Incubation Time:10 min
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Result:Increased the level of RAS-GTP in a dose-dependent manner.
Increased the level of pERK1/2T202/Y204 at doses of 0.1 and 1 µM.
Chemical Information
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CAS No. 2245237-53-8
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Appearance Solid
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분자량 483.02
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화학식 C26H32ClFN6
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Color Off-white to light yellow
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SMILES
CN1CCN(C2=C3C(N(CC4=CC(C)=C(F)C(C)=C4)C(N5CC6(CNC6)C5)=N3)=CC(Cl)=C2)CC1
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Synonyms
SOS1 activator 1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
용액&용해도
In Vitro:
DMSO : 10 mg/mL (20.70 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 (protect from 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 (protect from 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)
순도&문서
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Data Sheet (276 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
[1]. Timothy R Hodges, et al. Discovery and Structure-Based Optimization of Benzimidazole-Derived Activators of SOS1-Mediated Nucleotide Exchange on RAS. J Med Chem. 2018 Oct 11;61(19):8875-8894. [Content Brief]
[2]. Zhou C, et al. Discovery of the First-in-Class Agonist-Based SOS1 PROTACs Effective in Human Cancer Cells Harboring Various KRAS Mutations. J Med Chem. 2022 Mar 10;65(5):3923-3942. [Content Brief]
[3]. Stickler S, et al. Targeting KRAS in pancreatic cancer. Oncol Res. 2024 Apr 23;32(5):799-805. [Content Brief]
[4]. Hamilton G, et al. Targeting of SOS1: from SOS1 Activators to Proteolysis Targeting Chimeras. Curr Pharm Des. 2023;29(22):1741-1746. [Content Brief]
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 (protect from 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 | 2.0703 mL | 10.3515 mL | 20.7031 mL | 51.7577 mL |
| 5 mM | 0.4141 mL | 2.0703 mL | 4.1406 mL | 10.3515 mL | |
| 10 mM | 0.2070 mL | 1.0352 mL | 2.0703 mL | 5.1758 mL | |
| 15 mM | 0.1380 mL | 0.6901 mL | 1.3802 mL | 3.4505 mL | |
| 20 mM | 0.1035 mL | 0.5176 mL | 1.0352 mL | 2.5879 mL |
VUBI1 Related Classifications
HY-111671 Related Classifications
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