Description
The compound 9d induced SOS1 degradation in various KRAS-driven cancer cells and displayed superior antiproliferation activity compared to the agonist itself，9d induced the highly cooperative SOS1−9d−VCB complex formation. 9d achieved significant tumor growth inhibition in the xenograft mouse model bearing NCI-H358 cells with a good safety profile. These results collectively provide good evidence of using PROTAC 9d to study SOS1 biological functions and to develop a new class of pan-KRAS inhibitors for clinical use.
Product information
Molecular Weight: 1051.79
Formula: C57H76ClFN10O4S
Chemical Name: (2S,4R)-1-[(2S)-2-{9-[4-(6-chloro-2-{2,6-diazaspiro[3.3]heptan-2-yl}-1-[(4-fluoro-3,5-dimethylphenyl)methyl]-1H-1,3-benzodiazol-4-yl)piperazin-1-yl]nonanamido}-3,3-dimethylbutanoyl]-4-hydroxy-N-[(1S)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl]pyrrolidine-2-carboxamide
Smiles: CC(C)(C)[C@H](NC(=O)CCCCCCCCN1CCN(CC1)C1=CC(Cl)=CC2=C1N=C(N2CC1=CC(C)=C(F)C(C)=C1)N1CC2(CNC2)C1)C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)C1C=CC(=CC=1)C1SC=NC=1C
InChiKey: AZBRWXRYNYEDKG-VWELVXIZSA-N
InChi: InChI=1S/C57H76ClFN10O4S/c1-36-24-40(25-37(2)49(36)59)29-69-46-27-43(58)26-45(50(46)64-55(69)67-33-57(34-67)31-60-32-57)66-22-20-65(21-23-66)19-13-11-9-8-10-12-14-48(71)63-52(56(5,6)7)54(73)68-30-44(70)28-47(68)53(72)62-38(3)41-15-17-42(18-16-41)51-39(4)61-35-74-51/h15-18,24-27,35,38,44,47,52,60,70H,8-14,19-23,28-34H2,1-7H3,(H,62,72)(H,63,71)/t38-,44+,47-,52+/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shelf Life: ≥12 months if stored properly.
Products are for research use only. Not for human use.
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