VVD-849
Based on 1 Customer Validation
VVD-849 is a RAS ligand. VVD-849 covalently binds to Cys242 in the RAS-binding domain of PI3K p110α and promotes RAS/PI3K interaction. VVD-849 partially inhibits pAKT (S473) in HER2-overexpressing tumors. VVD-849 can be used for the research of cancers such as breast cancer.
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- Purity: 99.76%
- CAS No.: 3055321-14-4
- 화학식: C29H31ClFN3O6S2
- 분자량:636.15
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보관:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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
- 순도&문서
- References
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Help & FAQs
Biological Activity
VVD-849 (2 µM; 2 h) exhibits excellent selectivity for cysteine residues in live Jurkat cells[1].
VVD-849 (4 h) enhances the interaction between KRASG12C and p110α in HEK293T cell lysates (cotransfected with p85α), with an IC50 of 0.02 µM[1].
VVD-849 (30 min) increases the level of pAKTS473 in H358 cells, with an IC50 of 0.04 µM[1].
VVD-849 (2 h) partially inhibits the level of pAKT (S473) in N87 (HER2-overexpressing) cells[1].
VVD-849 (1 h) binds to p110α C242 in Jurkat cell lysates, with a TE50 of 0.063 µM[1].
VVD-849 (1 h) shows binding to p110α C242 in Jurkat cell lysates as detected by pocket probe assay, with a TE50 of 0.1 µM[1].
VVD-849 partially inhibits AKT phosphorylation in HER2-overexpressing human gastric cancer N87 cells, which may result from its combined stimulatory effect on the RAS-p110α interaction and inhibitory effect on the HER2-mediated PI3Kα signaling pathway[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3055321-14-4
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Appearance Solid
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분자량 636.15
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화학식 C29H31ClFN3O6S2
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Color White to off-white
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SMILES
ClC1=CC(C2=CC(OCC3=NC=CC=C3)=CC=C2)=C(S(N4CCC(C(N[C@@H](C)/C=C\S(C)(=O)=O)=O)(F)CC4)(=O)=O)C=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
용액&용해도
DMSO : 500 mg/mL (785.98 mM; Need ultrasonic and warming; 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 (stored under nitrogen). 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 (stored under nitrogen). 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 (273 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]. Klebba JE, et al. Covalent inhibitors of the RAS binding domain of PI3Kα impair tumor growth driven by RAS and HER2. bioRxiv [Preprint]. 2024 Dec 20:2024.12.17.629001. [Content Brief]
[2]. Klebba JE, et al. Covalent inhibitors of the PI3Kα RAS binding domain impair tumor growth driven by RAS and HER2. Science. 2025 Nov 13;390(6774):702-709. [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 (stored under nitrogen). 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 | 1.5720 mL | 7.8598 mL | 15.7196 mL | 39.2989 mL |
| 5 mM | 0.3144 mL | 1.5720 mL | 3.1439 mL | 7.8598 mL | |
| 10 mM | 0.1572 mL | 0.7860 mL | 1.5720 mL | 3.9299 mL | |
| 15 mM | 0.1048 mL | 0.5240 mL | 1.0480 mL | 2.6199 mL | |
| 20 mM | 0.0786 mL | 0.3930 mL | 0.7860 mL | 1.9649 mL | |
| 25 mM | 0.0629 mL | 0.3144 mL | 0.6288 mL | 1.5720 mL | |
| 30 mM | 0.0524 mL | 0.2620 mL | 0.5240 mL | 1.3100 mL | |
| 40 mM | 0.0393 mL | 0.1965 mL | 0.3930 mL | 0.9825 mL | |
| 50 mM | 0.0314 mL | 0.1572 mL | 0.3144 mL | 0.7860 mL | |
| 60 mM | 0.0262 mL | 0.1310 mL | 0.2620 mL | 0.6550 mL | |
| 80 mM | 0.0196 mL | 0.0982 mL | 0.1965 mL | 0.4912 mL | |
| 100 mM | 0.0157 mL | 0.0786 mL | 0.1572 mL | 0.3930 mL |
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