A selective ERK1/2 inhibitor
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GDC-0994

Item No. 21107

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[(1S)-1-(4-chloro-3-fluorophenyl)-2-hydroxyethyl]-4-[2-[(1-methyl-1H-pyrazol-5-yl)amino]-4-pyrimidinyl]-2(1H)-pyridinone
CAS Number
1453848-26-4
Synonyms
  • RG-7842
Molecular Formula
C21H18ClFN6O2
Formula Weight
440.9
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mLDMSO: 30 mg/mLDMSO:PBS (pH 7.2)(1:9): 0.10 mg/mLEthanol: 30 mg/mL
λmax
220, 332 nm
SMILES
O=C(N([C@H](CO)C1=CC(F)=C(Cl)C=C1)C=C2)C=C2C3=NC(NC4=CC=NN4C)=NC=C3
InChi Code
InChI=1S/C21H18ClFN6O2/c1-28-19(5-8-25-28)27-21-24-7-4-17(26-21)13-6-9-29(20(31)11-13)18(12-30)14-2-3-15(22)16(23)10-14/h2-11,18,30H,12H2,1H3,(H,24,26,27)/t18-/m1/s1
InChi Key
RZUOCXOYPYGSKL-GOSISDBHSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $36

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    1 mg

    $63

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    5 mg

    $253

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    10 mg

    $469

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    Product Description

    GDC-0994 is a potent and selective ERK1 and ERK2 inhibitor with IC50 values of 6.1 and 4.1 nM, respectively.1 It inhibits ERK-dependent p90RSK serine 380 phosphorylation in PMA-stimulated HepG2 cells with an IC50 value of 12 nM. GDC-0994 inhibited growth of HCT116 human colorectal cancer xenograft tumors by 49%, 57%, and 80% at 30, 60, and 100 mg/kg, respectively, when administered orally once daily for 21 days.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Blake, J.F., Burkard, M.E., Chan, J., et al. Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an extracellular signal-regulated kinase ½ (ERK1/2) inhibitor in early clinical development. J. Med. Chem. 59(12), 5650-5660 (2016).