PROTAC SMARCA2 degrader-36
PROTAC SMARCA2 degrader-36 (Compound 26) is a selective and potent SMARCA2 PROTAC degrader with a DC50 of 51 nM. PROTAC SMARCA2 degrader-36 promotes ubiquitination and degradation of SMARCA2. PROTAC SMARCA2 degrader-36 exhibits anticancer activity against non-small cell lung cancer. PROTAC SMARCA2 degrader-36 can be used in studies related to SMARCA4-deficient cancers.
(Pink: SMARCA2 ligand (HY-181910); Blue: VHL ligand (HY-112078); Black: linker).
For research use only. We do not sell to patients.
- Formula: C42H49N7O6S
- Molecular Weight:779.95
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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VHL |
SMARCA2 |
Compound 26 (100 mg/kg; i.v.; single dose) induces sustained SMARCA2 degradation for up to 24 hours in NCI-H1944 xenograft tumors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude SCID (female)[1]
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Dosage:100 mg/kg
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Administration:i.v.; three times per week for 21 days or single
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Result:Achieved a tumor/control (T/C) ratio of 48.9% at 100 mg/kg.
Achieved a tumor/control (T/C) ratio of 63.9% at 50 mg/kg.
Showed no significant body weight loss.
Confirmed degradation of target protein SMARCA2.
Chemical Information
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Molecular Weight 779.95
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Formula C42H49N7O6S
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SMILES
O=C([C@H]1N(C([C@@H](NC(CN2CCC(C3=CC4=NN=C(C5=CC=CC=C5O)C=C4O3)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)N[C@H](C6=CC=C(C7=C(C)N=CS7)C=C6)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)