ALK/IGF1R inhibitor

Product Name: ALK/IGF1R inhibitor
CAS No.: 1356962-20-3
Chemical Name: ALK/IGF1R inhibitor
Synonyms: CS-729;AZD3463;AZD-3463;AZD 3463;AZD3463 AZD-3463;ALK/IGF1R inhibitor;AZD3463;AZD3463;AZD 3463;ALK/IGF1R inhibitor USP/EP/BP;AZD3463; AZD 3463; ALK/IGF1R INHIBITOR;N-[4-(4-Amino-1-piperidinyl)-2-methoxyphenyl]-5-chloro-4-(1H-indol-3-yl)-2-pyrimidinamine
CBNumber: CB32666595
Molecular Formula: C24H25ClN6O
Formula Weight: 448.95
MOL File: 1356962-20-3.mol

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ALK/IGF1R inhibitor Property

Boiling point:: 723.6±70.0 °C(Predicted)
Density: 1.338±0.06 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: insoluble in H2O; insoluble in EtOH; ≥11.22 mg/mL in DMSO
form: solid
pka: 14.62±0.30(Predicted)

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 26172
Product name: AZD 3463
Packaging: 5mg
Price: $109
Updated: 2024/03/01

Cayman Chemical

Product number: 26172
Product name: AZD 3463
Packaging: 25mg
Price: $381
Updated: 2024/03/01

Cayman Chemical

Product number: 26172
Product name: AZD 3463
Packaging: 1mg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 26172
Product name: AZD 3463
Packaging: 10mg
Price: $169
Updated: 2024/03/01

TRC

Product number: A808105
Product name: AZD3463
Packaging: 5mg
Price: $155
Updated: 2021/12/16

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ALK/IGF1R inhibitor Chemical Properties,Usage,Production

Uses

AZD3463, is a novel ALK/IGF1R dual Inhibitor, having the ability of overcoming multiple mechanisms of acquired resistance to Crizotinib (C785000).

Definition

ChEBI: AZD3463 is a member of the class of indoles that is 1H-indole substituted by a 2-[4-(4-aminopiperidin-1-yl)-2-methoxyanilino]-5-chloropyrimidin-4-yl group at position 3. It is an orally bioavailable dual inhibitor of ALK and IGF1R with Ki value of 0.75 nM for ALK. It has a role as an apoptosis inducer, an antineoplastic agent, an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor and an autophagy inducer. It is a member of indoles, an aminopiperidine, a monomethoxybenzene, an aminopyrimidine, a secondary amino compound, a tertiary amino compound and an organochlorine compound.

Biological Activity

azd3463 is a novel orally bioavailable alk/igf1r inhibitor with ki value of 0.75 nm. alk expression is largely restricted to neurons and upregulated in neuroblastoma. activated alk has been shown to promote cell survival and growth. high alk expression or mutations in the alk gene correlates with adverse outcomes in neuroblastoma. therefore, alk receptor tyrosine kinase is an important therapeutic target for drug development against neuroblastoma [1].

in vitro

azd3463 (5, 10, 20, and 50 μm) effectively inhibited the proliferation of neuroblastoma cell lines with wild type alk (wt) and alk activating mutations (f1174l and d1091n) via targeting the alk-mediated pi3k/akt/mtor pathway and ultimately induced apoptosis and autophagy in vitro. moreover, azd3463 (1 μm) significantly enhanced the cytotoxic effects of doxorubicin (1 μm) on neuroblastoma cells [1]. azd3463 simultaneously inhibited stat3 and akt to augment the cytotoxic effects of temozolomide and further reduce cell growth [2].

in vivo

azd3463 (15 mg/kg, i.p. injection) showed significant therapeutic efficacy on the growth of the neuroblastoma tumors with wt and f1174l oncogenic mutant alk in orthotopic xenograft mouse models [1].

target

alk, igf1r

IC 50

0.75 nm(ki)

References

1. wang y, wang l, guan s, cao w, wang h, chen z, et al. novel alk inhibitor azd3463 inhibits neuroblastoma growth by overcoming crizotinib resistance and inducing apoptosis. sci rep. 2016;6:19423. 2. sampson vb, vetter ns, kamara df, collier ab, gresh rc, kolb ea. vorinostat enhances cytotoxicity of sn-38 and temozolomide in ewing sarcoma cells and activates stat3/akt/mapk pathways. plos one. 2015;10(11):e0142704.

ALK/IGF1R inhibitor Preparation Products And Raw materials

Raw materials

Preparation Products

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ALK/IGF1R inhibitor Suppliers

China 95 United States 16 Global 111

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1356962-20-3, ALK/IGF1R inhibitorRelated Search:

AZD8186 AZD-0156 azd4635 AZD7986 Ceritinib N2-[2-Methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-N4-[2-[(1-methylethyl)sulfonyl]phenyl]-1,3,5-triazine-2,4-diamine 7-Ethyl-10-hydroxycamptothecin Vorinostat Erlotinib hydrochloride AP26113 1626387-81-2 AZD2098 AZD5153 AZD-7594 AZD-5582 AZD5153 AZD 7762 hydrochloride 1802148-05-5

AZD3463; AZD 3463; ALK/IGF1R INHIBITOR

CS-729

ALK/IGF1R inhibitor

AZD 3463

AZD3463

AZD-3463

N-[4-(4-Amino-1-piperidinyl)-2-methoxyphenyl]-5-chloro-4-(1H-indol-3-yl)-2-pyrimidinamine

2-Pyrimidinamine, N-[4-(4-amino-1-piperidinyl)-2-methoxyphenyl]-5-chloro-4-(1H-indol-3-yl)-

N-[4-(4-Amino-1-piperidinyl)-2-methoxyphenyl]-5-chloro-4-(1H-indol-3-yl)-2-pyrimidinamine AZD3463

AZD3463;AZD3463;AZD 3463

N-(4-(4-Aminopiperidin-1-yl)-2-methoxyphenyl)-5-chloro-4-(1H-indol-3-yl)pyrimidin-2-amine

ALK/IGF1R inhibitor USP/EP/BP

AZD3463 AZD-3463

1356962-20-3

Inhibitors