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Art. -Nr.: HY-152145

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PROTAC SOS1 degrader-3

PROTAC SOS1 degrader-3 is a PROTAC degrader targeting SOS1, which induces the targeted degradation of SOS1 via the ubiquitin-proteasome system, with DC₅₀ values ranging from 0.19 μM to 0.75 μM in multiple distinct colorectal cancer cell lines. PROTAC SOS1 degrader-3 inhibits the phosphorylation of AKT and ERK. PROTAC SOS1 degrader-3 induces apoptosis and morphological changes in KRAS-mutant colorectal cancer organoids. PROTAC SOS1 degrader-3 can be applied in studies related to kras-mutant colorectal cancer.
(Pink: SOS1 ligand (HY-125817); Blue: Cereblon ligand (HY-W039233); Black: linker).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 3029320-99-5
Formel: C₃₄H₃₂F₃N₇O₆
Molecular Weight:691.66

Speicherung:

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

Data Sheet (283 KB)

PROTAC SOS1 degrader-3 Chemical Structure

CAS. Nr.: 3029320-99-5

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Preis

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Menge

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

PROTAC SOS1 degrader-3 is a PROTAC degrader targeting SOS1, which induces the targeted degradation of SOS1 via the ubiquitin-proteasome system, with DC₅₀ values ranging from 0.19 μM to 0.75 μM in multiple distinct colorectal cancer cell lines. PROTAC SOS1 degrader-3 inhibits the phosphorylation of AKT and ERK. PROTAC SOS1 degrader-3 induces apoptosis and morphological changes in KRAS-mutant colorectal cancer organoids. PROTAC SOS1 degrader-3 can be applied in studies related to kras-mutant colorectal cancer^[1]. (Pink: SOS1 ligand (HY-125817); Blue: Cereblon ligand (HY-W039233); Black: linker).

IC₅₀ & Target

^[1]

SOS1

0.19-0.75 μM (DC₅₀)

Cereblon

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Ras Isoform-spezifische Produkte anzeigen :

Alle Akt Isoform-spezifische Produkte anzeigen :

Alle ERK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
SW-620	DC₅₀	0.59 μM	Concentration-dependent SOS1 degradation in SW620 human colorectal cancer cells after 24 h incubation measured by immunoblot assay. Concentration-dependent SOS1 degradation in SW620 human colorectal cancer cells after 24 h incubation measured by immunoblot assay.	36459180
HCT-116	DC₅₀	0.75 μM	Concentration-dependent SOS1 degradation in HCT116 human colorectal cancer cells after 24 h incubation measured by immunoblot assay. Concentration-dependent SOS1 degradation in HCT116 human colorectal cancer cells after 24 h incubation measured by immunoblot assay.	36459180
SW1417	DC₅₀	0.19 μM	Concentration-dependent SOS1 degradation in SW1417 human colorectal cancer cells after 24 h incubation measured by immunoblot assay. Concentration-dependent SOS1 degradation in SW1417 human colorectal cancer cells after 24 h incubation measured by immunoblot assay.	36459180

In Vitro

PROTAC SOS1 degrader-3 (compound P7) (0.01-10 μM; 3-48 h) induces robust time-dependent SOS1 degradation that reaches 92% at 48 h following treatment with 1 μM compound in SW620 colorectal cancer cells^[1].
PROTAC SOS1 degrader-3 (0.1-10 μM; 24 h) induces concentration-dependent SOS1 degradation in multiple distinct colorectal cancer cell lines, with DC₅₀ values of 0.19 μM to 0.75 μM at the 24 h timepoint^[1].
Targeted SOS1 protein degrader-3 (1 μM; 24-72 h) effectively degrades SOS1 and inhibits the viability of SOS1 inhibitor-sensitive KRAS-mutant colorectal cancer patient-derived organoid models, with IC₅₀ values ranging from 0.48 μM to 1.4 μM^[1].
PROTAC SOS1 degrader-3 (1 μM) in SW620 cells is fully mediated by the canonical cereblon E3 ligase / ubiquitin-proteasome degradation pathway^[1].
PROTAC SOS1 degrader-3 (1 μM; 24 h) demonstrates exceptional specificity for SOS1 degradation with no off-target degradation of canonical cereblon neosubstrate proteins in SW620 cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

SW620 human colorectal cancer cells
Concentration:

1 μM (time course); 0.01 μM, 0.1 μM, 1 μM, 10 μM (6 h time point)
Incubation Time:

3 h, 6 h, 12 h, 24 h, 48 h (1 μM); 6 h (0.1-10 μM)
Result:

Achieved 64% degradation of SOS1 after 6 h of 1 μM treatment.
Reached 92% maximum SOS1 degradation at 48 h of 1 μM treatment.

Western Blot Analysis^[1]

Cell Line:

SW620, HCT116, C2BB, and SW1417 human colorectal cancer cell lines
Concentration:

0.1 μM, 1 μM, 10 μM
Incubation Time:

24 h
Result:

Induced concentration-dependent SOS1 degradation across all four tested CRC cell lines.
Calculated DC50 values after 24 h treatment as 0.59 μM for SW620, 0.75 μM for HCT116, and 0.19 μM for SW1417.
Reached maximum SOS1 degradation of 87% for SW620, 76% for HCT116, and 83% for SW1417 at 10 μM after 24 h.

Chemical Information

CAS. Nr. 3029320-99-5
Molecular Weight 691.66
Formel C₃₄H₃₂F₃N₇O₆
SMILES

NC1=CC(C(F)(F)F)=CC([C@H](NC2=C3C=C(OC)C(OCC(NC4=CC=CC(C5=O)=C4CN5C(C(N6)=O)CCC6=O)=O)=CC3=NC(C)=N2)C)=C1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 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)

Verweise

[1]. Bian Y, et al. Development of SOS1 Inhibitor-Based Degraders to Target -Mutant Colorectal Cancer. Journal of medicinal chemistry. 2022 Dec 22;65(24):16432-16450. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise

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PROTAC SOS1 degrader-3

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Ras Isoform-spezifische Produkte anzeigen

Alle Akt Isoform-spezifische Produkte anzeigen

Alle ERK Isoform-spezifische Produkte anzeigen