An ERK inhibitor
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ASTX029

Item No. 33557

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(αR)-6-[5-chloro-2-[(tetrahydro-2H-pyran-4-yl)amino]-4-pyrimidinyl]-N-[(1S)-1-(3-fluoro-5-methoxyphenyl)-2-hydroxyethyl]-1,3-dihydro-α-methyl-1-oxo-2H-isoindole-2-acetamide
CAS Number
2095719-92-7
Molecular Formula
C29H31ClFN5O5
Formula Weight
584.0
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 15 mg/ml
λmax
223, 253 nm
SMILES
O=C1C2=CC(C3=NC(NC4CCOCC4)=NC=C3Cl)=CC=C2CN1[C@H](C)C(N[C@@H](C5=CC(OC)=CC(F)=C5)CO)=O
InChi Code
InChI=1S/C29H31ClFN5O5/c1-16(27(38)34-25(15-37)19-9-20(31)12-22(10-19)40-2)36-14-18-4-3-17(11-23(18)28(36)39)26-24(30)13-32-29(35-26)33-21-5-7-41-8-6-21/h3-4,9-13,16,21,25,37H,5-8,14-15H2,1-2H3,(H,34,38)(H,32,33,35)/t16-,25-/m1/s1
InChi Key
BVRGQPJKSKKGIH-PUAOIOHZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $69

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    1 mg

    $127

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    5 mg

    $591

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    10 mg

    $918

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    Product Description

    ASTX029 is an ERK inhibitor (IC50 = 2.7 nM for ERK2).1 It is selective for ERK over a panel of 465 kinases. ASTX029 reduces phosphorylation of p90 ribosomal S6 kinase (RSK) in mutant B-RAF-expressing A375 melanoma and mutant K-Ras-expressing HCT116 colorectal cancer cells with IC50 values of 3.3 and 4 nM, respectively. It inhibits proliferation in a panel of cancer cell lines, including melanoma, colorectal, and lung cancer cells. ASTX029 reduces tumor growth in A375, Calu-6, and COLO 205 mouse xenograft models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Munck, J., Berdini, V., Courtin, A., et al. The clinical candidate, ASTX029, is a novel, dual mechanism ERK1/2 inhibitor and has potent activity in MAPK-activated cancer cell lines and in vivo tumor models. Eur. J. Cancer 138(Suppl 2), S53 (2020).