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AT13148
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AT13148图片
CAS NO:1056901-62-2
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)313.78
FormulaC17H16ClN3O
CAS No.1056901-62-2
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 62 mg/mL (197.59 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Other info

Synonym: AT-13148; AT 13148; AT13148; AT13148 hydrochloride; AT13148 HCl

InChi Key: IIRWNGPLJQXWFJ-KRWDZBQOSA-N

InChi Code: InChI=1S/C17H16ClN3O/c18-16-7-5-15(6-8-16)17(22,11-19)14-3-1-12(2-4-14)13-9-20-21-10-13/h1-10,22H,11,19H2,(H,20,21)/t17-/m0/s1

SMILES Code: ClC1=CC=C([C@](C2=CC=C(C3=CNN=C3)C=C2)(O)CN)C=C1

Chemical Name(S)-1-(4-(1H-pyrazol-4-yl)phenyl)-2-amino-1-(4-chlorophenyl)ethanol
实验参考方法

In Vitro

Kinase Assay: AT13148 is assayed against 40 kinases and the percentage inhibition at 10 μM of AT13148 is determined. Individual IC50 values are measured for selected kinases using ATP concentrations equivalent to the Km for each enzyme.

Cell Assay: Cytotoxicity is determined using a 72 h Alamar Blue assay or a 96 h SRB assay. Cell lines: MES-SA, MES-SA/Dx5, BT474, HCT-116, A549, PC3, SK-BR-3, MCF7, U87MG, MDA-MB-468, DU-145, and SK-OV-3 cell lines; Incubation Time: 72 hours or 96 hours

AT13148, as a multi-AGC kinase inhibitor, potently inhibits proliferation with GI50 values of 1.5 to 3.8 μM across a selected panel of cancer cell lines with deregulation of PI3K-AKT-mTOR or RAS-RAF pathways. In PTEN-deficient MES-SA cells, AT13148 also inhibits AKT and p70S6K signaling.

In Vivo

AT13148 (50 mg/kg p.o.) markedly inhibits the activity of both AKT and p70S6K AGC kinases, and subsequently exhibits marked antitumor effects in human tumor xenografts.

Animal model

Athymic mice bearing MES-SA, BT474, or PC3 tumor xenografts

Formulation & Dosage

Dissolved in 10% DMSO, 1% Tween-20, and 89% saline; 50 mg/kg; p.o.

References

[1] Yap TA, et al. Clin Cancer Res. 2012, 18(14), 3912-3923.