A monovalent direct degrader of BRD4
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

PLX3618

Item No. 45519

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(6S)-2,3,9-trimethyl-4-[3′-[(pyrazolo[1,5-a]pyrimidin-3-ylcarbonyl)amino][1,1′-biphenyl]-4-yl]-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide
CAS Number
2851986-76-8
Molecular Formula
C32H27N9O2S
Formula Weight
601.7
Purity
≥98%
Formulation (Request formulation change)
A solid
SMILES
CC1=C(C)C(C(C2=CC=C(C3=CC(NC(C4=C5N(C=CC=N5)N=C4)=O)=CC=C3)C=C2)=N[C@H](C6=NN=C(N67)C)CC(N)=O)=C7S1
InChi Code
InChI=1S/C32H27N9O2S/c1-17-18(2)44-32-27(17)28(37-25(15-26(33)42)30-39-38-19(3)41(30)32)21-10-8-20(9-11-21)22-6-4-7-23(14-22)36-31(43)24-16-35-40-13-5-12-34-29(24)40/h4-14,16,25H,15H2,1-3H3,(H2,33,42)(H,36,43)/t25-/m0/s1
InChi Key
KGEBVZGNEUJHIO-VWLOTQADSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    1 mg

    $99

    Add

    5 mg

    $396

    Add

    10 mg

    $693

    Add
    Cayman Chemical
    Visit Our Cancer Resource Center
    Find Tools & Resources to Study the Hallmarks of Cancer
    • Cancer cell signaling & regulation
    • Cancer metabolism
    • Tumor microenvironment
    EXPLORE NOW
    Product Description

    PLX3618 is a monovalent direct degrader of bromodomain-containing protein 4 (BRD4).1 It binds to both bromodomain 1 (BD1) and BD2 of BRD4 and mediates its degradation via recruitment of the E3 ubiquitin ligase DDB1- and CUL4-associated factor 11 (DCAF11) with a half-maximal degradation concentration (DC50) value of 12.2 nM. PLX3618 inhibits the proliferation of a variety of hematopoietic cancer cells and induces apoptosis in MV4-11 acute myeloid leukemia (AML) cells. It induces tumor regression and intratumoral BRD4 degradation in an MV4-11 mouse xenograft model when administered at a dose of 5 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Parker, G.S., Toth, J.I., Fish, S., et al. Discovery of monovalent direct degraders of BRD4 that act via the recruitment of DCAF11. Mol. Cancer Ther. 23(10), 1446-1458 (2024).