An ALK and MET inhibitor
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X-376

Item No. 21341

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-[(4-methyl-1-piperazinyl)carbonyl]phenyl]-3-pyridazinecarboxamide
CAS Number
1365267-27-1
Molecular Formula
C25H25Cl2FN6O3
Formula Weight
547.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mLDMF:PBS(pH 7.2)(1:6): 0.14DMSO: 14 mg/mLEthanol: 5 mg/mL
λmax
244, 296 nm
SMILES
ClC1=C([C@H](OC2=C(N)N=NC(C(NC3=CC=C(C(N4CCN(C)CC4)=O)C=C3)=O)=C2)C)C(Cl)=CC=C1F
InChi Code
InChI=1S/C25H25Cl2FN6O3/c1-14(21-17(26)7-8-18(28)22(21)27)37-20-13-19(31-32-23(20)29)24(35)30-16-5-3-15(4-6-16)25(36)34-11-9-33(2)10-12-34/h3-8,13-14H,9-12H2,1-2H3,(H2,29,32)(H,30,35)/t14-/m1/s1
InChi Key
ONPGOSVDVDPBCY-CQSZACIVSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $153

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    10 mg

    $268

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    25 mg

    $587

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    Product Description

    X-376 is an inhibitor of anaplastic lymphoma kinase (ALK) and MET (IC50s = 0.61 and 0.69 nM, respectively).1 It selectively inhibits the growth of cancer cell lines harboring gain-of-function ALK-fusion proteins (IC50s = 32-150 nM) over those with cell growth driven by other mutant kinases (IC50s = 1,427->3,000 nM). X-376 (50 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).