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PROTAC K-Ras Degrader-4 (Compound 4) is a proteolysis-targeting chimera (PROTAC) molecule designed to selectively degrade oncogenic mutants of K-Ras, effectively degrading KRASG12D in the GP5d cell line and KRASG12V in SW620 cells with DC50 of 1 nM and 13 nM, respectively; it concomitantly inhibits the downstream MAPK signaling pathway and represents a novel therapeutic strategy for cancer research targeting previously undruggable Ras mutations.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $159 | - | In Stock | |
| 2 mg | $239 | - | In Stock | |
| 5 mg | $393 | - | In Stock | |
| 10 mg | $645 | - | In Stock | |
| 25 mg | $997 | - | In Stock | |
| 50 mg | $1,330 | - | In Stock |
| Description | PROTAC K-Ras Degrader-4 (Compound 4) is a proteolysis-targeting chimera (PROTAC) molecule designed to selectively degrade oncogenic mutants of K-Ras, effectively degrading KRASG12D in the GP5d cell line and KRASG12V in SW620 cells with DC50 of 1 nM and 13 nM, respectively; it concomitantly inhibits the downstream MAPK signaling pathway and represents a novel therapeutic strategy for cancer research targeting previously undruggable Ras mutations. |
| In vitro | PROTAC K-Ras Degrader-4 (0-1 μM, 5 days) was used to treat GP2d cell lines and was found to inhibit the expression of DUSP6 and the proliferation of GP2d cells with KRASG12D mutation. [1] |
| Molecular Weight | 989.22 |
| Formula | C50H60N12O6S2 |
| Cas No. | 2938169-99-2 |
| Smiles | C[C@]1(C2=C(SC(N)=C2C#N)CCC1)C3=NC(=NO3)C4=NC(=NC=C4)N5[C@@H](C)CN(CCCCOC=6C=C([C@H](C(=O)N7[C@H](C(NCC8=CC=C(C=C8)C9=C(C)N=CS9)=O)C[C@@H](O)C7)C(C)C)ON6)CCC5 |
| Relative Density. | no data available |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 80 mg/mL (80.87 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
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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