PROTAC BRD9 Degrader-8
PROTAC BRD9 Degrader-8 is a selective, orally active BRD9 PROTAC degrader with a DC50 of 16 pM.\nPROTAC BRD9 Degrader-8 induces cell cycle arrest at the G1 phase and promotes apoptosis. PROTAC BRD9 Degrader-8 can be used for research on acute myeloid leukemia and diffuse large B-cell lymphoma.
(Pink: BRD9 ligand (HY-175915); Blue: Cereblon ligand (HY-W585171); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 3081180-48-2
- Formula: C46H49N5O6
- Molecular Weight:767.91
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Biological Activity
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BRD9 16 pM (DC50) |
PROTAC BRD9 Degrader-8 (Compound E5) (7 days) potently inhibits proliferation of MV4-11, MOLM13, Kasumi-1, and OCI-LY10 hematological tumor cells with IC50 values ranging from 0.27 nM to 1.13 nM, with activity dependent on CRBN expression, and exhibits weaker activity in SU-DHL-2, SU-DHL-6, and U937 cells[1].
PROTAC BRD9 Degrader-8 (compound E5) (24 h) induces G1 phase cell cycle arrest in MV4-11 cells after 24 h of treatment[1].
PROTAC BRD9 Degrader-8 (compound E5) (0.01-10 nM; 48 h) dose-dependently induces apoptosis in MV4-11 cells after 48 h of treatment, with significant apoptosis observed at concentrations as low as 0.01 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV4-11 acute myeloid leukemia cells
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Concentration:0.01, 0.1, 1 and 10 nM
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Incubation Time:24 h
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Result:Induced cell cycle arrest at the G1 phas
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Cell Line:MV4-11 acute myeloid leukemia cells
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Concentration:0.01, 0.1, 1 and 10 nM
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Incubation Time:48 h
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Result:Induced cell apoptosis.
PROTAC BRD9 Degrader-8 (30 mg/kg; p.o.; once daily; for 18 consecutive days) inhibits tumor growth of OCI-LY10 diffuse large B-cell lymphoma xenografts in mice to 40% of that in the vehicle control group, with no observed toxicity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice[1]
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Dosage:20 mg/kg
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Administration:i.p.; daily; 19 days
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Result:Completely degraded BRD9 protein in tumor tissue relative to vehicle controls.
Achieved 30.92% tumor growth inhibition (TGI).
Reduced mean tumor volume to 766 mm3 vs 1187 mm3 in vehicle group.
Reduced mean relative tumor volume to 4.99 vs 7.85 in vehicle group.
Reduced mean tumor weight to 0.90 g vs 1.30 g in vehicle group.
Caused no significant weight loss or behavioral abnormalities in treated mice.
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Animal Model:Balb/c mice[1]
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Dosage:30 mg/kg
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Administration:p.o.; daily; 18 days
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Result:Reduced mean tumor volume to 309 mm3 vs 561 mm3 in vehicle group.
Reduced mean relative tumor volume to 4.00 vs 9.07 in vehicle group.
Achieved a tumor growth ratio (T/C%) of approximately 40%.
Reduced mean tumor weight to 0.56 g vs 1.12 g in vehicle group.
Caused no significant weight fluctuation or mortality in treated mice.
Chemical Information
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CAS No. 3081180-48-2
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Molecular Weight 767.91
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Formula C46H49N5O6
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SMILES
O=C1C2=C(C(C3=CC(OC)=C(C(OC)=C3)CN4CCC(CN5CCC(CC5)C6=C7C(C8=CC=C7)=C(C=C6)N(C9C(NC(CC9)=O)=O)C8=O)CC4)=CN1C)C=CC=C2
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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)
PROTAC BRD9 Degrader-8 Related Classifications
HY-162651 Related Classifications
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