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Cat. No.: HY-168637

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SIAIS562055

SIAIS562055 is a potent cereblon-based SOS1 PROTAC with a K_d of 95.9 nM. SIAIS562055 exhibits sustained degradation of SOS1 and inhibition of downstream ERK pathways. SIAIS562055 effectively blocked the binding of KRAS^G12C or KRAS^G12D 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); Blue: Cereblon ligand (HY-W586108); Black: linker (HY-W009145)).

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

CAS No.: 3062106-15-1
Formula: C₄₉H₆₂F₃N₇O₅S
Molecular Weight:918.12

Storage:

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

Data Sheet (267 KB)

SIAIS562055 Chemical Structure

CAS No.: 3062106-15-1

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

SIAIS562055 is a potent cereblon-based SOS1 PROTAC with a K_d of 95.9 nM. SIAIS562055 exhibits sustained degradation of SOS1 and inhibition of downstream ERK pathways. SIAIS562055 effectively blocked the binding of KRAS^G12C or KRAS^G12D to SOS1, with the IC₅₀ values of 95.7 nM and 134.5 nM, respectively. SIAIS562055 exhibits potent anticancer activity^[1]. (Pink: SOS1 ligand (HY-168638); Blue: Cereblon ligand (HY-W586108); Black: linker (HY-W009145)).

IC₅₀ & Target^[1]

Cereblon

SOS1

95.9 nM (Kd)

All PROTACs Isoforms :

All Ras Isoforms :

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.

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.

Chemical Information

CAS No. 3062106-15-1
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (267 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Ziwei Luo, et al. Targeted Degradation of SOS1 Exhibits Potent Anticancer Activity and Overcomes Resistance in KRAS-Mutant Tumors and BCR-ABL-Positive Leukemia. Cancer Res. 2024 Oct 22. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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SIAIS562055

All PROTACs Isoforms

All Ras Isoforms