A PROTAC that drives FAK degradation
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.

PROTAC FAK Degrader-1

Item No. 45149

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(4R)-3-methyl-N-[3-[2-[4-[[4-[[[3-[methyl(methylsulfonyl)amino]phenyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]phenoxy]ethoxy]-1-oxopropyl]-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-L-prolinamide
CAS Number
2301916-69-6
Synonyms
  • PROTAC Focal Adhesion Kinase Degrader-1
  • Proteolysis-trageting Chimera FAK Degrader-1
  • Proteolysis-trageting Chimera Focal Adhesion Kinase Degrader-1
Molecular Formula
C47H56F3N9O8S2
Formula Weight
996.1
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Sparingly soluble: 1-10 mg/ml
SMILES
O=C(N(C[C@@H]1O)[C@@H](C1)C(NCC2=CC=C(C(SC=N3)=C3C)C=C2)=O)[C@H](C(C)(C)C)NC(CCOCCOC(C=C4)=CC=C4NC(N=C5NCC6=CC(N(C)[S](C)(=O)=O)=CC=C6)=NC=C5C(F)(F)F)=O
InChi Code
InChI=1S/C47H56F3N9O8S2/c1-29-40(68-28-54-29)32-12-10-30(11-13-32)24-52-43(62)38-23-35(60)27-59(38)44(63)41(46(2,3)4)56-39(61)18-19-66-20-21-67-36-16-14-33(15-17-36)55-45-53-26-37(47(48,49)50)42(57-45)51-25-31-8-7-9-34(22-31)58(5)69(6,64)65/h7-17,22,26,28,35,38,41,60H,18-21,23-25,27H2,1-6H3,(H,52,62)(H,56,61)(H2,51,53,55,57)/t35-,38+,41-/m1/s1
InChi Key
MVULIYLBRNHLEE-LFHXYJAASA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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

    $29

    Add

    5 mg

    $123

    Add

    10 mg

    $189

    Add

    25 mg

    $363

    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

    PROTAC FAK degrader-1 is a proteolysis-targeting chimera (PROTAC) containing a derivative of the focal adhesion kinase (FAK) inhibitor defactinib (Item No. 17737) conjugated to VHL ligand 1 (Item No. 21591) via an alkyl ether linker.1 PROTAC FAK degrader-1 reduces the migration and invasion of MDA-MB-231 cells when used at concentrations of 50 and 100 nM, respectively.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Cromm, P.M., Samarasinghe, K.T.G., Hines, J., et al. Addressing kinase-independent functions of Fak via PROTAC-mediated degradation. J. Am. Chem. Soc. 140(49), 17019-17026 (2018).