2. PROTAC MAPK/ERK Pathway GPCR/G Protein
  3. PROTACs Ras
  4. SIAIS562055

SIAIS562055 is a potent cereblon-based SOS1 PROTAC with a Kd of 95.9 nM. SIAIS562055 exhibits sustained degradation of SOS1 and inhibition of downstream ERK pathways. SIAIS562055 effectively blocked the binding of KRASG12C or KRASG12D to SOS1, with the IC50 values of 95.7 nM and 134.5 nM, respectively. SIAIS562055 exhibits potent anticancer activity. (Pink: SOS1 ligand (HY-168638); Black: linker (HY-W539874); Blue: E3 ligase ligand (HY-W076696)).

For research use only. We do not sell to patients.

SIAIS562055 Chemical Structure

SIAIS562055 Chemical Structure

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SIAIS562055 Related Antibodies

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Description

SIAIS562055 is a potent cereblon-based SOS1 PROTAC with a Kd of 95.9 nM. SIAIS562055 exhibits sustained degradation of SOS1 and inhibition of downstream ERK pathways. SIAIS562055 effectively blocked the binding of KRASG12C or KRASG12D to SOS1, with the IC50 values of 95.7 nM and 134.5 nM, respectively. SIAIS562055 exhibits potent anticancer activity. (Pink: SOS1 ligand (HY-168638); Black: linker (HY-W539874); Blue: E3 ligase ligand (HY-W076696))[1].

IC50 & Target[1]

Cereblon

 

SOS1

95.9 nM (Kd)

In Vitro

SIAIS562055 (10-1000 nM; 24 h) exhibits sustained degradation of SOS1 and inhibition of downstream ERK pathways, resulting in superior anti-proliferative activity compared to small molecule inhibitors[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SIAIS562055 Related Antibodies

Western Blot Analysis[1]

Cell Line: NCI-H358 and GP2d cells
Concentration: 10 nM, 100 nM, 1000 nM
Incubation Time: 24 h
Result: Exhibited sustained degradation of SOS1 and inhibition of downstream ERK pathways.
In Vivo

SIAIS562055 (20-50 mg/kg; ip; daily; for 3 weeks) displays a promising antitumor potency in KRAS-mutant xenografts[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/c mice (6-7-week-old) injected with MIA PaCa-2 cells[1]
Dosage: 20 mg/kg; 40 mg/kg; 50 mg/kg
Administration: ip; daily; for 3 weeks
Result: Displayed promising antitumor potency.
Molecular Weight

918.12

Formula

C49H62F3N7O5S
SMILES

COC1=CC2=C(C(N[C@@H](C3=CC(N)=CC(C(F)(F)F)=C3)C)=NC(C)=N2)C=C1OC4CCN(CC4)CCCCCCCCCCCCSC5=C6C(C(N(C6)C7C(NC(CC7)=O)=O)=O)=CC=C5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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SIAIS562055 Related Classifications

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Help & FAQs
  • 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:

SIAIS562055SIAIS 562055SIAIS-562055PROTACsRasPROTAC SOS1 degraderKRASG12DKRASG12CERK pathwaysInhibitorinhibitorinhibit

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