A dual ERK1 and ERK5 inhibitor
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ADTL-EI1712

Item No. 30602

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[(2-chlorobenzoyl)amino]-6-[[(2-chlorophenyl)amino]thioxomethyl]-4,5,6,7-tetrahydro-thieno[2,3-c]pyridine-3-carboxamide
CAS Number
2414916-45-1
Molecular Formula
C22H18Cl2N4O2S2
Formula Weight
505.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 1 mg/mlDMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml
SMILES
O=C(C1=C(NC(C2=CC=CC=C2Cl)=O)SC3=C1CCN(C(NC4=CC=CC=C4Cl)=S)C3)N
InChi Code
InChI=1S/C22H18Cl2N4O2S2/c23-14-6-2-1-5-12(14)20(30)27-21-18(19(25)29)13-9-10-28(11-17(13)32-21)22(31)26-16-8-4-3-7-15(16)24/h1-8H,9-11H2,(H2,25,29)(H,26,31)(H,27,30)
InChi Key
LVSFMPVPLIMFMY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    25 mg

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    Product Description

    ADTL-EI1712 is a dual inhibitor of ERK1 and ERK5 (IC50s = 40.43 and 64.5 nM, respectively).1 It reduces ERK1 and ERK5 activity by 93.5% and 89.4%, respectively, but also inhibits ERK2 activity by 92.7%, in a panel of 100 kinases at 1 µM. ADTL-EI1712 inhibits proliferation of HL-60 and MKN74, but not HeLa, cancer cells (IC50s = 1.26, 2.55, and >50 µM, respectively). It reduces tumor growth and intratumor phosphorylation of ERK1/2 and ERK5 in an MKN74 mouse xenograft model when administered at a dose of 50 mg/kg per day.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wang, G., Zhao, Y., Liu, Y., et al. Discovery of a novel dual-target inhibitor of ERK1 and ERK5 that induces regulated cell death to overcome compensatory mechanism in specific tumor types. J. Med. Chem. 63(8), 3976-3995 (2020).