A potent, ATP-uncompetitive inhibitor of MEK1
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GDC-0623

Item No. 19479

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[(2-fluoro-4-iodophenyl)amino]-N-(2-hydroxyethoxy)-imidazo[1,5-a]pyridine-6-carboxamide
CAS Number
1168091-68-6
Molecular Formula
C16H14FIN4O3
Formula Weight
456.2
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlDMSO:PBS(pH 7.2) (1:4): 0.20 mg/mlEthanol: 1 mg/ml
λmax
282, 360 nm
SMILES
IC1=CC(F)=C(NC2=C(C(NOCCO)=O)C=CC3=CN=CN23)C=C1
InChi Code
InChI=1S/C16H14FIN4O3/c17-13-7-10(18)1-4-14(13)20-15-12(16(24)21-25-6-5-23)3-2-11-8-19-9-22(11)15/h1-4,7-9,20,23H,5-6H2,(H,21,24)
InChi Key
RFWVETIZUQEJEF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $46

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    5 mg

    $134

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    10 mg

    $222

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    25 mg

    $333

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    Product Description

    GDC-0623 is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki = 0.13 nM in the presence of ATP).1 It inhibits the proliferation of A375 BRAF(V600E) and HCT116 KRAS(G13D)-mutant cancer cell lines with EC50 values of 7 and 42 nM, respectively.1 GDC-0623 inhibits ERK and BIM phosphorylation resulting in upregulation and stabilization of pro-apoptotic BIM protein in KRAS mutant and wild-type HCT116 cells and in KRAS mutant GW620 cells.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hatzivassiliou, G., Haling, J.R., Chen, H., et al. Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers. Nature 501(7466), 232-236 (2013).

    2. Zaanan, A., Okamoto, K., Kawakami, H., et al. The mutant KRAS gene up-regulates BCL-XL protein via STAT3 to confer apoptosis resistance that is reversed by BIM protein induction and BCL-XL antagonism. The Journal of Biological Chemisty 290(39), 23838-23849 (2015).