An EML4-ALK inhibitor
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EML4-ALK Kinase Inhibitor 1

Item No. 45387

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-ethyl-5-[(trans-4-methoxycyclohexyl)amino]-3-[[3-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]amino]-2-pyrazinecarboxamide
CAS Number
1373409-08-5
Molecular Formula
C31H48N8O3
Formula Weight
580.8
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Ethanol: Slightly Soluble: 0.1-1 mg/ml
SMILES
CN1CCN(C2CCN(C(C=CC(NC3=NC(N[C@@H]4CC[C@H](CC4)OC)=C(N=C3C(N)=O)CC)=C5)=C5OC)CC2)CC1
InChi Code
InChI=1S/C31H48N8O3/c1-5-25-30(33-21-6-9-24(41-3)10-7-21)36-31(28(35-25)29(32)40)34-22-8-11-26(27(20-22)42-4)39-14-12-23(13-15-39)38-18-16-37(2)17-19-38/h8,11,20-21,23-24H,5-7,9-10,12-19H2,1-4H3,(H2,32,40)(H2,33,34,36)/t21-,24-
InChi Key
KBHZCRDGGWIHQF-SAIGFBBZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $95

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    5 mg

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    Product Description

    EML4-ALK kinase inhibitor 1 is an inhibitor of the anaplastic lymphoma kinase (ALK) fusion protein EML4-ALK (IC50 = 1 nM).1 It inhibits the growth of Ba/F3 cells expressing EML4-ALK (IC50 = 9.7 nM). In vivo, EML4-ALK kinase inhibitor 1 (10 mg/kg) induces tumor regression in mice xenografted with NIH3T3 cells expressing EML4-ALK.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Iikubo, K., Kurosawa, K., Matsuya, T., et al. Synthesis and structure-activity relationships of pyrazine-2-carboxamide derivatives as novel echinoderm microtubule-associated protein-like 4 (EML4)-anaplastic lymphoma kinase (ALK) inhibitors. Bioorg. Med. Chem. 27(8), 1683-1692 (2019).