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Cat. No.: HY-144657

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(4S)-PROTAC SOS1 degrader-1

(4S)-PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 degrader. (4S)-PROTAC SOS1 degrader-1 decreases the expression of pERK and RAS-GTP level in a dose-dependent manner. (4S)-PROTAC SOS1 degrader-1 significantly inhibits the tumor growth in vivo.
(Pink: SOS1 ligand (HY-111671); Blue: VHL ligand (HY-184855); Black: linker).

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

CAS No.: 2913176-81-3
Formula: C₅₇H₇₆ClFN₁₀O₄S
Molecular Weight:1051.79

Storage:

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

Data Sheet (273 KB)

(4S)-PROTAC SOS1 degrader-1 Chemical Structure

CAS No.: 2913176-81-3

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Use of MCE Products

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
Classifications
Bioz

Biological Activity

Description

(4S)-PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 degrader. (4S)-PROTAC SOS1 degrader-1 decreases the expression of pERK and RAS-GTP level in a dose-dependent manner. (4S)-PROTAC SOS1 degrader-1 significantly inhibits the tumor growth in vivo^[1]. (Pink: SOS1 ligand (HY-111671); Blue: VHL ligand (HY-184855); Black: linker).

IC₅₀ & Target^[1]

K-RAS

All PROTACs Isoforms :

All Ras Isoforms :

In Vitro

(4S)-PROTAC SOS1 degrader-1 (compound 9d) (0.1, 1 μM) shows a potent SOSI degradation activity with an SOS1 protein degradation of 56.2 and 92.5% at 0.1 and 1 μM in NCI-H358 cells, respectively^[1].
(4S)-PROTAC SOS1 degrader-1 (24 h) degrades SOS1 in a dose- and time-dependent manner in NCI-H358 cells^[1].
(4S)-PROTAC SOS1 degrader-1 (9.8-2500 nM; 24 h) does not induce SOS2 and KRAS degradation in NCI-H358 cells^[1].
(4S)-PROTAC SOS1 degrader-1 (7.8-2000 nM; 24 h) decreases the expression of pERK and RAS-GTP level in NCI-H358 cells in a dose-dependent manner^[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 cells
Concentration:

7.8, 15.6, 31.2, 62.5, 125, 250, 500, 1000, 2000 nM
Incubation Time:

24 h
Result:

Showed a potent degradation activity with an EC₅₀ of 98.4 nM in NCI-H358 cells.

RT-PCR^[1]

Cell Line:

NCI-H358 cells
Concentration:

1 µM
Incubation Time:

24, 48, 72 h
Result:

Showed the SOS2 mRNA level remained constant during the incubation period.

Cell Proliferation Assay^[1]

Cell Line:

NCI-H358, MIA PaCa2, AsPC-1, SK-LU-1, SW620, A549 cells
Concentration:

0-10000 nM
Incubation Time:

7 days
Result:

Inhibited the cell growth with IC₅₀s of 0.525, 0.218, 0.307, 0.115, 0.199, 0.232 µM (EC₅₀s of 0.098, 0.255, 0.119, 0.104, 0.125, 0.022 µM)for NCI-H358, MIA PaCa2, AsPC-1, SK-LU-1, SW620, A549 cells, respectively.

In Vivo

PROTAC SOS1 degrader-2 (10, 20 mg/kg; i.p., daily for 21 days ) significantly inhibits the tumor growth in vivo with a good safety profile^[1].

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

Animal Model:

BALB/c nude mice (NCI-H358 tumor xenografts)^[1]
Dosage:

10, 20 mg/kg
Administration:

I.p.; daily, 21 days
Result:

Significantly inhibited the tumor growth in vivo with a good safety profile.

Chemical Information

CAS No. 2913176-81-3
Molecular Weight 1051.79
Formula C₅₇H₇₆ClFN₁₀O₄S
SMILES

O=C(N[C@@H](C(C)(C)C)C(N1C[C@@H](O)C[C@H]1C(N[C@@H](C)C2=CC=C(C3=C(C)N=CS3)C=C2)=O)=O)CCCCCCCCN4CCN(CC4)C5=C6N=C(N7CC8(CNC8)C7)N(CC9=CC(C)=C(F)C(C)=C9)C6=CC(Cl)=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 (273 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]. Zhou C,et al. Discovery of the First-in-Class Agonist-Based SOS1 PROTACs Effective in Human Cancer Cells Harboring Various KRAS Mutations. J Med Chem. 2022; 65(5):3923-3942. [Content Brief]

Calculators

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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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MOQ

Minimum order quantity

100 mg

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

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(4S)-PROTAC SOS1 degrader-1

All PROTACs Isoforms

All Ras Isoforms