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Danusertib(PHA739358)
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。
Danusertib(PHA739358)图片
CAS NO:827318-97-8
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)474.55
FormulaC26H30N6O3
CAS No.827318-97-8
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 95 mg/mL (200.2 mM)
Water:<1 mg/mL (slightly soluble or insoluble)
Ethanol: <1 mg/mL (slightly soluble or insoluble)
Solubility (In vivo)1% DMSO+30% polyethylene glycol+1% Tween 80: 30mg/mL
Chemical Name/Synonyms

Synonym: Danusertib; PHA-739358; PHA 739358; PHA739358;

Chemical Name: (R)-N-(5-(2-methoxy-2-phenylacetyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)-4-(4-methylpiperazin-1-yl)benzamide

InChi Key: XKFTZKGMDDZMJI-HSZRJFAPSA-N

InChi Code: InChI=1S/C26H30N6O3/c1-30-12-14-31(15-13-30)20-10-8-19(9-11-20)25(33)27-24-21-16-32(17-22(21)28-29-24)26(34)23(35-2)18-6-4-3-5-7-18/h3-11,23H,12-17H2,1-2H3,(H2,27,28,29,33)/t23-/m1/s1

SMILES Code: O=C(NC1=NNC2=C1CN(C([C@H](OC)C3=CC=CC=C3)=O)C2)C4=CC=C(N5CCN(C)CC5)C=C4

实验参考方法
In VitroDanusertib inhibits the activities of other kinases such as FGFR1, Abl, Ret and Trka, with IC50 of 47 nM, 25 nM, 31 nM and 31 nM, respectively. In a cell assay, after treatment of wild-type and p53-deficient MEFs with Danusertib, the wild-type cells undergo an arrest in mitosis (4N) that is maintained for up to 48 h.
In VivoAdministration of 25 mg/kg Danusertib (b.d. i.v.) to HL-60 xenograft rats results in 75% inhibition of tumor growth with complete regression in one animal. Danusertib significantly inhibits proliferation of K562 cells and virtually suppressed tumor growth during the 10-day treatment period.
Animal modelFemale SCID mice
Formulation & Dosage DMSO; 15 mg/kg; i.p.
References[1] Gontarewicz A, et al. Blood, 2008, 111(8), 4355-4364.
生物活性




Inhibition of cellular pathways by PHA-739358. Mol Cancer Ther. 2007 Dec;6(12 Pt 1):3158-68.


PHA-739358 treatment results in the inhibition of tumor growth in TRAMP mice as assessed by MRI evaluation. Mol Cancer Ther. 2007 Dec;6(12 Pt 1):3158-68.