Fig. 1 · Structure
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Setidegrasib
KRAS G12D PROTAC Degrader
Setidegrasib is a PROTAC degrader specifically targeting the KRAS G12D mutation with a DC50 of 37 nM. This compound effectively induces the degradation of KRAS G12D protein, leading to the suppression of key signaling molecules such as p-ERK, p-AKT, and p-S6 in AsPC-1 cells. Setidegrasib demonstrates significant anti-tumor activity across various cancer xenograft models, making it a valuable tool for studying KRAS(G12D)-mutated solid tumors.
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Specifications
| Manufacturer | Adooq Bioscience |
|---|---|
| Actions | Degrader |
| CAS Number | 2821793-99-9 |
| Applications | KRAS G12D PROTAC Degrader |
| Formula | C60H65FN12O7S |
| Molecular Weight | 1117.30 |
| Synonyms | ASP-3082; KRAS G12D inhibitor 17 |
| SMILES | CC1=C(SC=N1)C2=CC=C(C=C2)[C@@H](NC([C@@H]3C[C@H](CN3C([C@H](C(C)C)N4C=C(N=N4)C5=CC=C(C=C5)COC6=[C@]([C@]7=C(C(F)=CC8=C7C=NN8)C)C(C9CC9)=CC%10=C6N=C(N=C%10N%11C[C@@H]%12C[C@H]%11CN%12)OC%13CCOCC%13)=O)O)=O)CO |
Storage & Solubility
In Vitro Solubility
Reported Solubility
No reported solubility data are available for this product.
Preparing Stock Solutions
| Concentration | |
|---|---|
Values use four significant digits. Prepare to the final solution volume; this is not the volume of solvent to add.
Stock preparation is unavailable for this product molecular weight.
Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.
Storage
Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.