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Merck
CN

SML2590

AZD3463

≥98% (HPLC)

Synonym(s):

AZD 3463, AZD-3463, N-(4-(4-Aminopiperidin-1-yl)-2-methoxyphenyl)-5-chloro-4-(1H-indol-3-yl)pyrimidin-2-amine, N-[4-(4-Amino-1-piperidinyl)-2-methoxyphenyl]-5-chloro-4-(1H-indol-3-yl)-2-pyrimidinamine

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About This Item

Empirical Formula (Hill Notation):
C24H25ClN6O
CAS Number:
1356962-20-3
Molecular Weight:
448.95
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD25976759

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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)

SMILES string

ClC1=CN=C(N=C1C2=CNC3=C2C=CC=C3)NC4=CC=C(C=C4OC)N5CCC(CC5)N

InChI key

GCYIGMXOIWJGBU-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

−20°C

Biochem/physiol Actions

AZD3463 is an orally available, potent receptor tyrosine kinase (RTK) inhibtor against anaplastic lymphoma kinase ALK (Ki = 0.75 nM; IC50 = 15-21 nM with 5FAM-Srctide as substrate & 30 μM ATP), insulin-like growth factor (IGF)-1 receptor (IGF1R), ROS1 (c-Ros), and Trk-A (NTRK1). AZD3463 effectively inhibits multiple crizotinib-resistant cancer growth and displays in vivo efficacy against FLT3-ITD-dependent MOLM-13 acute myeloid leukemia (AML) as well as NGP (wt ALK) & SH-SY5Y (ALK-F1174L) neuroblastoma in mice (15 mg/kg ip.).
Orally available, potent RTK inhibtor against anaplastic lymphoma kinase (ALK), IGF1R, ROS1 and Trk-A (NTRK1) with in vitro and in vivo anticancer efficacy.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
0000068918
0000068919
0000063776

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