WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 206039
CAS#: 1356962-20-3
Description: AZD-3463 is a potent ALK/IGF1R inhibitor with potential anticancer activity. AZD3463 inhibits neuroblastoma growth by overcoming crizotinib resistance and inducing apoptosis. AZD3463 effectively suppressed the proliferation of NB cell lines with wild type ALK (WT) as well as ALK activating mutations (F1174L and D1091N) by blocking the ALK-mediated PI3K/AKT/mTOR pathway and ultimately induced apoptosis and autophagy. In addition, AZD3463 enhanced the cytotoxic effects of doxorubicin on NB cells. AZD3463 also exhibited significant therapeutic efficacy on the growth of the NB tumors with WT and F1174L activating mutation ALK in orthotopic xenograft mouse models.
MedKoo Cat#: 206039
Name: AZD-3463
CAS#: 1356962-20-3
Chemical Formula: C24H25ClN6O
Exact Mass: 448.17784
Molecular Weight: 448.95
Elemental Analysis: C, 64.21; H, 5.61; Cl, 7.90; N, 18.72; O, 3.56
Synonym: AZD3463; AZD 3463; AZD-3463.
IUPAC/Chemical Name: N-(4-(4-aminopiperidin-1-yl)-2-methoxyphenyl)-5-chloro-4-(1H-indol-3-yl)pyrimidin-2-amine.
InChi Key: GCYIGMXOIWJGBU-UHFFFAOYSA-N
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)
SMILES Code: ClC1=CN=C(NC2=CC=C(N3CCC(N)CC3)C=C2OC)N=C1C4=CNC5=C4C=CC=C5
Appearance: Light green to green solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 448.95 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Wang Y, Wang L, Guan S, Cao W, Wang H, Chen Z, Zhao Y, Yu Y, Zhang H, Pang JC,
Huang SL, Akiyama Y, Yang Y, Sun W, Xu X, Shi Y, Zhang H, Kim ES, Muscal JA, Lu
F, Yang J. Novel ALK inhibitor AZD3463 inhibits neuroblastoma growth by
overcoming crizotinib resistance and inducing apoptosis. Sci Rep. 2016 Jan
20;6:19423. doi: 10.1038/srep19423. PubMed PMID: 26786851; PubMed Central PMCID:
PMC4726162.
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 Nov 16;10(11):e0142704. doi:
10.1371/journal.pone.0142704. PubMed PMID: 26571493; PubMed Central PMCID:
PMC4646493.