An ALK and IGF-1R inhibitor
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AZD 3463

Item No. 26172

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-(4-amino-1-piperidinyl)-2-methoxyphenyl]-5-chloro-4-(1H-indol-3-yl)-2-pyrimidinamine
CAS Number
1356962-20-3
Molecular Formula
C24H25ClN6O
Formula Weight
449.0
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 2.5 mg/mlDMSO: 3.3 mg/ml
λmax
212, 276, 321 nm
SMILES
ClC1=CN=C(NC2=C(OC)C=C(N3CCC(N)CC3)C=C2)N=C1C4=CNC5=C4C=CC=C5
InChi Code
InChI=1S/C24H25ClN6O/c1-32-22-12-16(31-10-8-15(26)9-11-31)6-7-21(22)29-24-28-14-19(25)23(30-24)18-13-27-20-5-3-2-4-17(18)20/h2-7,12-15,27H,8-11,26H2,1H3,(H,28,29,30)
InChi Key
GCYIGMXOIWJGBU-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature 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

    AZD 3463 is an inhibitor of anaplastic lymphoma kinase (ALK) and the insulin growth factor-1 receptor (IGF-1R).1 It inhibits ALK with an IC50 value of 15 nM.2 It inhibits the proliferation of neuroblastoma cells with wild-type (WT) ALK (IC50s = 2.8-21.3 µM) and ALK with the activating mutations ALKF1174L and ALKD1091N (IC50s = 1.7 and 16.49 µM, respectively) and induces apoptosis and autophagy.1 It reduces tumor growth in neuroblastoma mouse xenograft models expressing WT ALK or the ALKF1174L mutation when administered at a dose of 15 mg/kg per day for 21 days.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wang, Y., Wang, L., Guan, S., et al. Novel ALK inhibitor AZD3463 inhibits neuroblastoma growth by overcoming crizotinib resistance and inducing apoptosis. Sci. Rep. 6:19423, (2016).

    2. Aquila, B., Kamhi, V., Peng, B., et al. Preparation of substituted pyrimidinamines as ALK kinase inhibitors. US20120028924A1, 1-54 (2012).