A potent inhibitor of B-Raf
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CEP-32496

Item No. 18776

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-[(6,7-dimethoxy-4-quinazolinyl)oxy]phenyl]-N'-[5-(2,2,2-trifluoro-1,1-dimethylethyl)-3-isoxazolyl]-urea
CAS Number
1188910-76-0
Molecular Formula
C24H22F3N5O5
Formula Weight
517.5
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMF:PBS(pH7.2) (1:2): 0.3 mg/mlDMSO: 20 mg/mlEthanol: 2 mg/ml
λmax
239, 319 nm
SMILES
COC1=C(OC)C=C(C(OC2=CC=CC(NC(NC3=NOC(C(C)(C)C(F)(F)F)=C3)=O)=C2)=NC=N4)C4=C1
InChi Code
InChI=1S/C24H22F3N5O5/c1-23(2,24(25,26)27)19-11-20(32-37-19)31-22(33)30-13-6-5-7-14(8-13)36-21-15-9-17(34-3)18(35-4)10-16(15)28-12-29-21/h5-12H,1-4H3,(H2,30,31,32,33)
InChi Key
DKNUPRMJNUQNHR-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $49

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    1 mg

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    5 mg

    $329

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    10 mg

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    Product Description

    CEP-32496 is a potent inhibitor of B-RafV600E (Kd = 14 nM in an in vitro binding assay).1 It blocks B-RafV600E-dependent phosphorylation of MEK in human melanoma A375 and colorectal cancer COLO 205 cells (IC50s = 78 and 60 nM, respectively).1 CEP-32496 binds kinases other than B-Raf but displays selective cytotoxicity for cells expressing B-RafV600E.1 It displays good oral bioavailability in rats, dogs, and monkeys and has single oral dose pharmacodynamics inhibition of both pMEK and pERK in B-RafV600E colon carcinoma xenografts in nude mice.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. James, J., Ruggeri, B., Armstrong, R.C., et al. CEP-32496: a novel orally active BRAFV600E inhibitor with selective cellular and in vivo antitumor activity. Mol. Cancer Ther. 11(4), 930-941 (2012).