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Cat. No.: HY-161173

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PROTAC SOS1 degrader-5

Name: PROTAC SOS1 degrader-5
Brand: MedChemExpress
SKU: HY-161173
Availability: PreOrder

PROTAC SOS1 degrader-5 is a potent SOS1 PROTAC degrader with a DC₅₀ value of 13 nM. PROTAC SOS1 degrader-5 induces CRBN-dependent ubiquitination and degradation of SOS1 protein, inhibits the proliferation of KRAS^G12C-mutated cancer cells, and suppresses tumor growth in xenograft models. PROTAC SOS1 degrader-5 can be used in studies related to KRAS^G12C-mutated non-small cell lung cancer.
(Pink: SOS1 ligand (HY-175891); Blue: Cereblon ligand (HY-10984); Black: linker).

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

CAS No.: 2836273-61-9
Formula: C₄₅H₅₁F₃N₈O₇
Molecular Weight:872.93

Storage:

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

Data Sheet (280 KB)

PROTAC SOS1 degrader-5 Chemical Structure

CAS No.: 2836273-61-9

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Fluorescent Dye

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

Biological Activity
- Description
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

PROTAC SOS1 degrader-5 is a potent SOS1 PROTAC degrader with a DC₅₀ value of 13 nM. PROTAC SOS1 degrader-5 induces CRBN-dependent ubiquitination and degradation of SOS1 protein, inhibits the proliferation of KRAS^G12C-mutated cancer cells, and suppresses tumor growth in xenograft models. PROTAC SOS1 degrader-5 can be used in studies related to KRAS^G12C-mutated non-small cell lung cancer^[1]. (Pink: SOS1 ligand (HY-175891); Blue: Cereblon ligand (HY-10984); Black: linker).

All PROTACs Isoforms :

All Ras Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
DLD-1	IC₅₀	63 nM Compound: 4	Antiproliferative activity against human DLD-1 cells harboring G13D mutant assessed as inhibition of cell proliferation incubated for 7 days by celltiter-glo 3D assay Antiproliferative activity against human DLD-1 cells harboring G13D mutant assessed as inhibition of cell proliferation incubated for 7 days by celltiter-glo 3D assay	[PMID: 38206836]
NCI-H358	IC₅₀	5 nM Compound: 4	Antiproliferative activity against human NCI-H358 cells assessed as inhibition of cell proliferation incubated for 7 days by celltiter-glo 3D assay Antiproliferative activity against human NCI-H358 cells assessed as inhibition of cell proliferation incubated for 7 days by celltiter-glo 3D assay	[PMID: 38206836]
NCI-H358	IC₅₀	5 nM Compound: 4	Antiproliferative activity against human NCI-H358 cells harboring G12C mutant assessed as inhibition of cell proliferation incubated for 7 days by celltiter-glo 3D assay Antiproliferative activity against human NCI-H358 cells harboring G12C mutant assessed as inhibition of cell proliferation incubated for 7 days by celltiter-glo 3D assay	[PMID: 38206836]
NCI-H441	IC₅₀	43 nM Compound: 4	Antiproliferative activity against human NCI-H441 cells harboring G12V mutant assessed as inhibition of cell proliferation incubated for 7 days by celltiter-glo 3D assay Antiproliferative activity against human NCI-H441 cells harboring G12V mutant assessed as inhibition of cell proliferation incubated for 7 days by celltiter-glo 3D assay	[PMID: 38206836]

In Vitro

OthersAnti-cancer

Others

PROTAC SOS1 degrader-5 (Compound 4) (1.37 nM-1 μM; 6 h) induces selective degradation of SOS1 (but not SOS2) protein in NCI-H358 cells via a CRBN-dependent ubiquitination pathway, with a DC₅₀ of 13 nM and a maximum degradation rate of 88%^[1].

Anti-cancer

PROTAC SOS1 degrader-5 (7 days) potently inhibits the proliferation of NCI-H358 (KRAS^G12C) cells, with an IC₅₀ value of 5 nM^[1].
PROTAC SOS1 degrader-5 (7 days) inhibits the proliferation of NCI-H441 (KRAS^G12V) cells with an IC₅₀ value of 43 nM^[1].
PROTAC SOS1 degrader-5 (7 days) inhibits the proliferation of DLD-1 (KRAS^G13D) cells with an IC₅₀ of 63 nM^[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
Concentration:

1.37, 4.12, 12.35, 37.04, 111.11, 333.33 nM; 1 μM
Incubation Time:

6 h
Result:

Induced significant SOS1 protein degradation with a DC₅₀ of 13 nM and achieved a maximum degradation (D_max) of 88%.
Observed a hook effect: degradation was optimal at 0.1 to 1 μM, and decreased at concentrations above 1 μM due to binary complex formation reducing ternary complex assembly.

Parmacokinetics

Species	Dose	Route	T_max	C_max	AUC_0-t	AUC_0-∞	T_1/2
Mice^[1]	10 mg/kg	i.p.	1 h	1868 ng/mL	4368 ng·h/mL	4378 ng·h/mL	4.05 h

In Vivo

Anti-cancer

PROTAC SOS1 degrader-5 (Compound 4) (30 mg/kg; i.p.; twice daily; 21 days) exhibits significant in vivo antitumor activity with a 58.8% tumor growth inhibition rate in BALB/c nude mice bearing NCI-H358 xenografts^[1].

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

Animal Model:

BALB/c nude mice^[1]
Dosage:

30 mg/kg
Administration:

i.p.; twice daily; 21 days
Result:

Achieved a tumor growth inhibition (TGI) rate of 58.8% relative to the vehicle control.
Exhibited no statistically significant body weight loss during the study.

Related Protocols :

Chemical Information

CAS No. 2836273-61-9
Molecular Weight 872.93
Formula C₄₅H₅₁F₃N₈O₇
SMILES

CC1=NC2=C(C=C(C(OC)=C2)OCC3(CN(C(CCCCCCNC4=CC=CC5=C4C(N(C5=O)C6CCC(NC6=O)=O)=O)=O)C)CC3)C(N[C@@H](C7=CC(N)=CC(C(F)(F)F)=C7)C)=N1
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 (280 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]. Pang X, et al. Discovery of Potent SOS1 PROTACs with Effective Antitumor Activities against NCI-H358 Tumor Cells In Vitro/In Vivo. J Med Chem. 2024 Jan 25;67(2):1563-1579. [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.

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