Danusertib(PHA739358)

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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。

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
Formula	C26H30N6O3
CAS No.	827318-97-8
Storage	-20℃ for 3 years in powder form
Storage	-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 Vitro	Danusertib 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 Vivo	Administration 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 model	Female 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.