PROTAC BRD3/BRD4-L degrader-2

Cat. No.: HY-149948: FAQs
Data Sheet Handling Instructions

Molarity Calculator

PROTAC BRD3/BRD4-L degrader-2 is a PROTAC molecule and can selectively degrade cellular BRD3 and BRD4-L with K_i 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.

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

PROTAC BRD3/BRD4-L degrader-2 Chemical Structure

Size		Stock
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote
Other size		Get quote

Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Featured Recommendations

•Related Small Molecules:

•Related Proteins:

View All PROTACs Isoform Specific Products:

View All Isoforms

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

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].

In Vitro

PROTAC BRD3/BRD4-L degrader-2 (Compound 28) has binding affinity for BRD3 BD1and BRD3 BD2 with K_i 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.

Western Blot Analysis^[1]

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.

In Vivo

PROTAC BRD3/BRD4-L degrader-2 (compound 28) (oral, i.v.; 3 mg/kg) has poor oral bioavailability and shows good systemic exposure when administered intravenously^[1].
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:

	T_max (h)	T_1/2(h)	C_max (ng/mL)	AUC_0-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.

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

Handling Instructions (2659 KB)

References

[1]. Yan Z, et al. Selective degradation of cellular BRD3 and BRD4-L promoted by PROTAC molecules in six cancer cell lines. Eur J Med Chem. 2023;254:115381. [Content Brief]