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NST-628 is a pan-RAF-MEK molecular glue that prevents RAF from phosphorylating and activating MEK, inhibiting the RAF-MEK signaling complex.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $199 | - | In Stock |
| Description | NST-628 is a pan-RAF-MEK molecular glue that prevents RAF from phosphorylating and activating MEK, inhibiting the RAF-MEK signaling complex. |
| In vitro | NST-628 demonstrates elevated antiproliferative activity in BRAF Class II/III mutant cell models compared to other RAF and MEK inhibitors, without promoting heterodimer formation of BRAF and CRAF. [1] NST-628 (4-100 nM; 48 h) induces early and late apoptosis in a dose-dependent manner and decreases live cell populations in NRAS mutant IPC-298 and SK-MEL-2, NF1 mutant MeWo, and KRAS mutant HCT116 cell lines. [1] |
| In vivo | NST-628 when administered orally (p.o.) at doses of 3 mg/kg and 5 mg/kg once daily (qd), or 1.5 mg/kg twice daily (b.i.d), significantly slowed tumor growth in models with KRAS and NRAS mutations. In the SK-MEL-2-luc model, it caused tumor regression. [1] Administered intragastrically (i.g.) at 0.3-3 mg/kg once daily for 18-20 days, NST-628 inhibited the RAS-MAPK pathway in mice in a dose-dependent manner, showing strong anti-tumor activity in the MeWo-luc model. At a dose of 2 mg/kg once daily for 26 days in an NCI-H23 KRASG12C-mutant lung adenocarcinoma model, NST-628 effectively slowed tumor growth and significantly inhibited the RAS-MAPK pathway. [1] |
| Synonyms | NST628, NST 628 |
| Molecular Weight | 488.46 |
| Formula | C22H18F2N4O5S |
| Cas No. | 3002056-30-3 |
| Smiles | O=C1OC=2C=C(OC3=NC=CC=C3F)C=CC2C(=C1CC=4C=CN=C(NS(=O)(=O)NC)C4F)C |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 80 mg/mL (163.78 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (6.76 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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