PROTAC SOS1 degrader-10

Cat. No.: HY-161654: Data Sheet Handling Instructions
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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))
(Pink: SOS1 ligand (HY-161655); Blue: Cereblon ligand (HY-W249500); Black: linker (HY-161656)).

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PROTAC SOS1 degrader-10 화학구조

CAS No. : 3043923-74-3

사이즈		재고
MOQ		Minimum order quantity
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100 mg		견적 받기
250 mg		견적 받기
Other size		견적 받기

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K-Ras H-Ras N-Ras Ras

Biological Activity
순도&문서
References
고객리뷰

제품 설명

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] (Pink: SOS1 ligand (HY-161655); Blue: Cereblon ligand (HY-W249500); Black: linker (HY-161656)).

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]

분자량

969.10

화학식

C₅₁H₆₃F₃N₁₀O₆

CAS No.

3043923-74-3

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

선적

Room temperature in continental US; may vary elsewhere.

보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Handling Instructions (2659 KB)

References

[1]. Wang, K, et al. “Design, synthesis, and bioevaluation of SOS1 PROTACs derived from pyrido[2,3-d]pyrimidin-7-one-based SOS1 inhibitor.” Bioorganic & medicinal chemistry letters vol. 107 (2024): 129780. [Content Brief]