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

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

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

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

CAS No. : 2913176-81-3

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(4S)-PROTAC SOS1 degrader-1 Related Antibodies

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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].

IC50 & Target[1]

K-RAS

 

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.

(4S)-PROTAC SOS1 degrader-1 Related Antibodies

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.
Molecular Weight

1051.79

Formula

C57H76ClFN10O4S
CAS No.
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
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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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(4S)-PROTAC SOS1 degrader-1 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:

(4S)-PROTAC SOS1 degrader-12913176-81-3PROTACsRasAntitumorNCI-H358 tumor xenograftsNCI-H358 cellspERKRAS-GTPKRASInhibitorinhibitorinhibit

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