PROTAC BRD3/BRD4-L degrader-2
PROTAC BRD3/BRD4-L degrader-2 is a PROTAC molecule and can selectively degrade cellular BRD3 and BRD4-L with Ki values of 16.91 and 2.8 nM, respectively. PROTAC BRD3/BRD4-L degrader-2 also has robust antitumor activity in mouse xenograft models. PROTAC BRD3/BRD4-L degrader-2 can be used for the research of cancer.
(Pink: BRD3 and BRD4-L ligand (HY-175924); Blue: Cereblon ligand (HY-138793); Black: linker).
For research use only. We do not sell to patients.
- Formula: C43H44ClN7O3
- Molecular Weight:742.31
-
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]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
All PROTACs Isoforms
More
Biological Activity
(Pink: BRD3 and BRD4-L ligand (HY-175924); Blue: Cereblon ligand (HY-138793); Black: linker).
Ki: 16.91 nM (BRD3 BD1); 2.8 nM (BRD3 BD2) [1].
IC50: 7.46 nM (MV4-11 cells); 85.4 nM (MM.1 S cells) [1].
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MM1.S | IC50 |
85.4 nM
Compound: 28; GXH71
|
Antiproliferative activity against human MM1.S cells assessed as cell growth inhibition measured after 4 days by CellTitre-Glo assay
Antiproliferative activity against human MM1.S cells assessed as cell growth inhibition measured after 4 days by CellTitre-Glo assay
|
[PMID: 37084596] |
| MV4-11 | IC50 |
7.46 nM
Compound: 28; GXH71
|
Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured after 3 days by CellTitre-Glo assay
Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured after 3 days by CellTitre-Glo assay
|
[PMID: 37084596] |
PROTAC BRD3/BRD4-L degrader-2 (Compound 28) has binding affinity for BRD3 BD1and BRD3 BD2 with Ki values of 16.91 and 2.8 nM, respectively[1].
PROTAC BRD3/BRD4-L degrader-2 has cellular activity in MV4-11 and MM.1 S cell lines with IC50 values of 7.46 and 85.4 nM, respectively[1].
PROTAC BRD3/BRD4-L degrader-2 (30 nM; 1, 3, 6, 8, 24 h) has a selective degradation effect for BRD3 and BRD4-L in a time-dependent manner[1].
PROTAC BRD3/BRD4-L degrader-2 (1, 3, 10, 30, 100, 300 nM; 24 h) has antitumor activity in MM.1 S cells and dosedependently induced cell cycle arrest at G1 phase[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:MM.1 S cells
-
Concentration:30 nM
-
Incubation Time:1, 3, 6, 8, 24 h
-
Result:Degraded BRD3 and BRD4-L in a time-dependent manner.
PROTAC BRD3/BRD4-L degrader-2 (i.v.; 3 mg/kg) has antitumor efficacy in MM.1 S mouse xenograft model[1].
PROTAC BRD3/BRD4-L degrader-2 (i.v.; 1, 5 mg/kg; signal dose) promotes selective degradation of BRD3 and BRD4-L in vivo and exhibits robust antitumor activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57 mice[1].
-
Dosage:3 mg/kg
-
Administration:Oral gavage; Intravenous injection
-
Result:
Tmax (h) T1/2(h) Cmax (ng/mL) AUC0-t (h×ng/mL) CL (mL/h/kg) F(%) i.v. 3 mg/kg 0.1 0.5 7414 ± 1765 2961 ± 314 1016 ± 114 p.o. 3 mg/kg 0.4 ± 0.1 na 51 ± 23 26 ± 8 74130 ± 44731 2.14
-
Animal Model:MM.1S mouse xenograft model[1].
-
Dosage:1, 5 mg/kg
-
Administration:i.v.; signal dose
-
Result:Inhibited tumor growth with 40% at 1 mg/kg and shows 64% tumor growth inhibition at 5 mg/kg.
Promoted selectively depletion of BRD3 and BRD4-L in tumor tissue for 1 mg/kg and 5 mg/kg.
Chemical Information
-
Molecular Weight 742.31
-
Formula C43H44ClN7O3
-
SMILES
CC1=NN=C2CCC(C3=C(N12)C=CC(C4=CC=C(C=C4)CN(C)CCCCC5=C6CN(C(C6=CC=C5)=O)C7CCC(NC7=O)=O)=C3)NC8=CC=C(C=C8)Cl
-
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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC BRD3/BRD4-L degrader-2 Related Classifications
HY-149948 Related Classifications
Powered by Bioz