An inhibitor of ERK1/2
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AZD 0364

Item No. 29827

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(6R)-7-[(3,4-difluorophenyl)methyl]-6,7-dihydro-6-(methoxymethyl)-2-[5-methyl-2-[(1-methyl-1H-pyrazol-5-yl)amino]-4-pyrimidinyl]-imidazo[1,2-a]pyrazin-8(5H)-one
CAS Number
2097416-76-5
Molecular Formula
C24H24F2N8O2
Formula Weight
494.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 16 mg/mlEthanol: 10 mg/ml
λmax
265, 324 nm
SMILES
O=C1N(CC2=CC=C(F)C(F)=C2)[C@@H](COC)CN3C1=NC(C4=NC(NC5=CC=NN5C)=NC=C4C)=C3
InChi Code
InChI=1S/C24H24F2N8O2/c1-14-9-27-24(30-20-6-7-28-32(20)2)31-21(14)19-12-33-11-16(13-36-3)34(23(35)22(33)29-19)10-15-4-5-17(25)18(26)8-15/h4-9,12,16H,10-11,13H2,1-3H3,(H,27,30,31)/t16-/m1/s1
InChi Key
HVIGNZUDBVLTLU-MRXNPFEDSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $107

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    5 mg

    $451

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    10 mg

    $740

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    Product Description

    AZD 0364 is an inhibitor of ERK2 (IC50 = <0.3 nM) that also inhibits ERK1.1 It is selective for ERK2 over MEK1 up to 10 µM and inhibits only four additional kinases by greater than 80% in a panel of 140 kinases at 1 µM but does inhibit ERK7, ARK5, Cdk5/p25, and Cdk5/p35 (IC50s = 30, 400, 300, and 300 nM, respectively). AZD 0364 inhibits cell growth in A549 non-small cell lung cancer cells (NSCLCs) when used in combination with AZD 6244 (Item No. 11599).2 It reduces tumor growth and induces regression in a Calu-6 mouse xenograft model when administered at doses of 15 and 50 mg/kg per day, respectively.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ward, R.A., Anderton, M.J., Bethel, P.A., et al. Discovery of a potent and selective oral inhibitor of ERK1/2 (AZD0364) that is efficacious in both monotherapy and combination therapy in models of nonsmall cell lung cancer (NSCLC). J. Med. Chem. 62(24), 11004-11018 (2019).

    2. Ward, R.A., Jones, C.D., Swallow, S., et al. Dihydroimidazopyrazinone derivatives useful in the treatment of cancer. (2017).