2. PROTAC MAPK/ERK Pathway GPCR/G Protein
  3. PROTACs Ras
  4. PROTAC SOS1 degrader-1

PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 degrader with an DC50 of 98.4 nM. PROTAC SOS1 degrader-1 shows antiproliferation activity in cancer cells with various KRAS mutations. PROTAC SOS1 degrader-1 shows antitumor effect with low toxicity.

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PROTAC SOS1 degrader-1

PROTAC SOS1 degrader-1 Chemical Structure

CAS No. : 2913185-35-8

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PROTAC SOS1 degrader-1 Related Antibodies

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Description

PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 degrader with an DC50 of 98.4 nM. PROTAC SOS1 degrader-1 shows antiproliferation activity in cancer cells with various KRAS mutations. PROTAC SOS1 degrader-1 shows antitumor effect with low toxicity[1].

IC50 & Target

DC50: 98.4 nM (SOS1)[1]
Cellular Effect
Cell Line Type Value Description References
A549 IC50
0.232 μM
Compound: 9d
Antiproliferative activity against human A549 cells harboring KRAS G12S mutant assessed as cell growth inhibition incubated for 7 days by CellTiter-Glo 3D cell viability assay
Antiproliferative activity against human A549 cells harboring KRAS G12S mutant assessed as cell growth inhibition incubated for 7 days by CellTiter-Glo 3D cell viability assay
[PMID: 35230841]
ASPC1 IC50
0.307 μM
Compound: 9d
Antiproliferative activity against human ASPC1 cells harboring KRAS G12D mutant assessed as cell growth inhibition incubated for 7 days by CellTiter-Glo 3D cell viability assay
Antiproliferative activity against human ASPC1 cells harboring KRAS G12D mutant assessed as cell growth inhibition incubated for 7 days by CellTiter-Glo 3D cell viability assay
[PMID: 35230841]
ASPC1 IC50
72.3 nM
Compound: 9d
Effect of compound on human ASPC1 cells harboring KRAS G12D mutant assessed as inhibition of ERK phosphorylation incubated for 24 hr by Western blot analysis
Effect of compound on human ASPC1 cells harboring KRAS G12D mutant assessed as inhibition of ERK phosphorylation incubated for 24 hr by Western blot analysis
[PMID: 35230841]
MIA PaCa-2 IC50
0.218 μM
Compound: 9d
Antiproliferative activity against human MIA PaCa-2 cells harboring KRAS G12C mutant assessed as cell growth inhibition incubated for 7 days by CellTiter-Glo 3D cell viability assay
Antiproliferative activity against human MIA PaCa-2 cells harboring KRAS G12C mutant assessed as cell growth inhibition incubated for 7 days by CellTiter-Glo 3D cell viability assay
[PMID: 35230841]
NCI-H358 IC50
0.525 μM
Compound: 9d
Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant assessed as growth inhibition incubated for 7 days by CellTiter-Glo 3D cell viability assay
Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant assessed as growth inhibition incubated for 7 days by CellTiter-Glo 3D cell viability assay
[PMID: 35230841]
SK-LU-1 IC50
0.115 μM
Compound: 9d
Antiproliferative activity against human SK-LU-1 cells harboring KRAS G12D mutant assessed as cell growth inhibition incubated for 7 days by CellTiter-Glo 3D cell viability assay
Antiproliferative activity against human SK-LU-1 cells harboring KRAS G12D mutant assessed as cell growth inhibition incubated for 7 days by CellTiter-Glo 3D cell viability assay
[PMID: 35230841]
SW-620 IC50
0.199 μM
Compound: 9d
Antiproliferative activity against human SW620 cells harboring KRAS G12V mutant assessed as cell growth inhibition incubated for 7 days by CellTiter-Glo 3D cell viability assay
Antiproliferative activity against human SW620 cells harboring KRAS G12V mutant assessed as cell growth inhibition incubated for 7 days by CellTiter-Glo 3D cell viability assay
[PMID: 35230841]
In Vitro

PROTAC SOS1 degrader-1 (compound 9d) (0.1, 1 μM) shows SOSI degradation activity with an SOS1 protein degradation of 56.2 and 92.5% at 0.1 and 1 μM, respectively[1].
PROTAC SOS1 degrader-1 (0-2000 nM; 24 h) exhibits SOS1 degradation activity with an DC50 of 98.4 nM in a dose- and time-dependent manner in NCI-H358 cells[1].
PROTAC SOS1 degrader-1 (0-2500 nM; 24 h) dose-dependently reduced the SOS1 protein level but showed no effect on SOS2 and KRAS up to 2.5 μM in NCI-H358 and AsPc-1 cells[1].
PROTAC SOS1 degrader-1 (0-2000 nM; 24 h) reduces the expression of KRAS-GTP, induced ERK phosphorylation with an IC50value of 72.3 nM, and significantly increases the pERK level after 6-24 h[1].

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

PROTAC SOS1 degrader-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: NCI-H358 cells
Concentration: 0-2000 nM
Incubation Time: 0-24 h
Result: Decreased the expression of SOS1 in a dose- and time-dependent manner in NCI-H358 cells.

RT-PCR[1]

Cell Line: NCI-H358 cells
Concentration: 1 µM
Incubation Time: 24, 48, 72 h
Result: Showed no effffect on SOS2 mRNA expression.

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: Showed anti-proliferation activity with an IC50s of 0.525, 0.218, 0.307, 0.115, 0.199, 0.232 µM and DC50s 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-1 (10 mg/kg; i.p.) shows good PK profile with low toxicity[1].
PROTAC SOS1 degrader-1 (0, 10, 20 mg/kg; i.p.; once a day for 3 weeks) shows significant anti-tumor activities in the xenograft mouse model[1].
Pharmacokinetic Parameters of PROTAC SOS1 degrader-1 in BALB/c mice[1].

compound dose (mg/kg) T1/2 (h) Tmax (h) Cmax (ng/mL) AUClast (h*ng/mL) AUCINF (h*ng/mL) MRTINF-obs(h)
9d 10 8.64±0.31 0.250v±0 1221±132 3895±335 4420±363 10.2±0.4
Male BALB/c mice; 10 mg/kg for i.p.[1].

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

Animal Model: Male BALB/c mice[1]
Dosage: 10 mg/kg (dissolved in solution containing dimethyl sulfoxide, PEG400, and 10% hydroxypropyl-β-cyclodextrin in water (5/5/90, v/v/v))
Administration: I.p.
Result: Showed good PK profile with high exposure (AUC0‑∞ = 4420 h*ng/mL) and maximum concentration (Cmax = 1221 ng/mL) in mouse plasma.
Animal Model: 6-8 weeks, BALB/c mice [1]
Dosage: 0, 10, 20 mg/kg
Administration: I.p.; once a day for a week
Result: Showed low toxicity for mouse.
Animal Model: 6-8 weeks, BALB/c nude mice (NCI-H358 tumor xenografts) [1]
Dosage: 0, 10, 20 mg/kg
Administration: I.p.; once a day for 3 weeks;
Result: Inhibited the tumor growth by 72.5 and 86.1% at 10 and 20 mg/kg, respectively.
Animal Model: 6-8 weeks, BALB/c nude mice (NCI-H358 tumor xenografts)[1]
Dosage: 0, 20, 50 mg/kg
Administration: Intratumoral injection; twice-weekly for 5 weeks
Result: Significantly prevented tumor growth in vivo with a good safety profile.
Molecular Weight

1051.79

Formula

C57H76ClFN10O4S
CAS No.
SMILES

O=C([C@H]1N(C([C@@H](NC(CCCCCCCCN2CCN(C3=C4C(N(CC5=CC(C)=C(F)C(C)=C5)C(N6CC7(CNC7)C6)=N4)=CC(Cl)=C3)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)N[C@H](C8=CC=C(C9=C(C)N=CS9)C=C8)C
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
References
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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:

PROTAC SOS1 degrader-12913185-35-8PROTACsRaslow toxicityanti-tumorNCI-H358 cellsanti-proliferationKRAS-GTPpERKxenografts modelKRAS MutationsInhibitorinhibitorinhibit

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