An ALK and MET inhibitor
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X-396

Item No. 44938

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-[[(3R,5S)-3,5-dimethyl-1-piperazinyl]carbonyl]phenyl]-3-pyridazinecarboxamide
CAS Number
1370651-20-9
Synonyms
  • Ensartinib
Molecular Formula
C26H27Cl2FN6O3
Formula Weight
561.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Slightly soluble: 0.1-1 mg/ml
SMILES
C[C@H](C1=C(C(F)=CC=C1Cl)Cl)OC2=C(N)N=NC(C(NC3=CC=C(C(N4C[C@@H](N[C@@H](C4)C)C)=O)C=C3)=O)=C2
InChi Code
InChI=1S/C26H27Cl2FN6O3/c1-13-11-35(12-14(2)31-13)26(37)16-4-6-17(7-5-16)32-25(36)20-10-21(24(30)34-33-20)38-15(3)22-18(27)8-9-19(29)23(22)28/h4-10,13-15,31H,11-12H2,1-3H3,(H2,30,34)(H,32,36)/t13-,14+,15-/m1/s1
InChi Key
GLYMPHUVMRFTFV-QLFBSQMISA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $35

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    5 mg

    $149

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    10 mg

    $228

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    25 mg

    $481

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    Product Description

    X-396 is an inhibitor of anaplastic lymphoma kinase (ALK) and MET (IC50s = <0.4 and 0.74 nM, respectively).1 It selectively inhibits the growth of cancer cell lines harboring gain-of-function ALK-fusion proteins (IC50s = 9-106 nM) over those with cell growth driven by other mutant kinases (IC50s = 757->3,000 nM). X-396 (25 mg/kg) reduces tumor growth in a lung cancer mouse xenograft model using NCI H3122 cells, which express a gain-of-function EML4-ALK fusion protein.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lovly, C.M., Heuckmann, J.M., de Stanchina, E., et al. Insights into ALK-driven cancers revealed through development of novel ALK tyrosine kinase inhibitors. Cancer Res. 71(14), 4920-4931 (2011).