2. PROTAC MAPK/ERK Pathway GPCR/G Protein
  3. SOS1 PROTACs Ras
  4. PROTAC SOS1 degrader-10

PROTAC SOS1 degrader-10 (Compound 11o) is a degrader for son of sevenless 1 (SOS1) in a CRBN and proteasome dependent manner. PROTAC SOS1 degrader-10 degrades SOS1 in KRAS mutant cancer cells SW620, A549 and DLD-1, with DC50s of 2.23, 1.85 and 7.53 nM, respectively. PROTAC SOS1 degrader-10 inhibits the proliferations of cells SW620, A549 and DLD-1, with IC50s of 36.7, 52.2 and 107 nM, respectively. PROTAC SOS1 degrader-10 inhibits phosphorylation of ERK. (Pink: SOS1 ligand (HY-161655); Black: linker (HY-161656); Blue: E3 ligase ligand (HY-W249500))

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PROTAC SOS1 degrader-10

PROTAC SOS1 degrader-10 Estructura química

No. CAS : 3043923-74-3

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PROTAC SOS1 degrader-10 Related Antibodies

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Descripciòn

PROTAC SOS1 degrader-10 (Compound 11o) is a degrader for son of sevenless 1 (SOS1) in a CRBN and proteasome dependent manner. PROTAC SOS1 degrader-10 degrades SOS1 in KRAS mutant cancer cells SW620, A549 and DLD-1, with DC50s of 2.23, 1.85 and 7.53 nM, respectively. PROTAC SOS1 degrader-10 inhibits the proliferations of cells SW620, A549 and DLD-1, with IC50s of 36.7, 52.2 and 107 nM, respectively. PROTAC SOS1 degrader-10 inhibits phosphorylation of ERK. (Pink: SOS1 ligand (HY-161655); Black: linker (HY-161656); Blue: E3 ligase ligand (HY-W249500))[1]

Cellular Effect
Cell Line Type Value Description References
A549 IC50
52.2 nM
Compound: 11o
Antiproliferative activity against human A549 cells harboring KRAS G12S mutant assessed as inhibition of cell growth
Antiproliferative activity against human A549 cells harboring KRAS G12S mutant assessed as inhibition of cell growth
[PMID: 38714262]
DLD-1 IC50
107 nM
Compound: 11o
Antiproliferative activity against human DLD-1 cells harboring KRAS G13D mutant assessed as inhibition of cell growth
Antiproliferative activity against human DLD-1 cells harboring KRAS G13D mutant assessed as inhibition of cell growth
[PMID: 38714262]
SW-620 IC50
36.7 nM
Compound: 11o
Antiproliferative activity against human SW620 cells harboring KRAS G12V mutant assessed as inhibition of cell growth
Antiproliferative activity against human SW620 cells harboring KRAS G12V mutant assessed as inhibition of cell growth
[PMID: 38714262]
Peso molecular

969.10

Fòrmula

C51H63F3N10O6
No. CAS
SMILES

NC1=CC(C(F)(F)F)=CC([C@@H](C)NC2=C3C(N(C)C(C([C@H]4CC[C@H](C(N5CCN(CC6CCC7(CCN(C(C8=CC=C(OC)C(N9CCC(NC9=O)=O)=C8)=O)CC7)CC6)CC5)=O)CC4)=C3)=O)=NC=N2)=C1
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PROTAC SOS1 degrader-10 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PROTAC SOS1 degrader-103043923-74-3SOS1PROTACsRasRas/Rac guanine nucleotide exchange factor 1SW620A549DLD-1KRAS mutantInhibitorinhibitorinhibit

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Nombre del producto:
PROTAC SOS1 degrader-10
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HY-161654
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