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product name Danusertib (PHA-739358)


ReferencesMol Cancer Ther. 2007 Dec;6(12 Pt 1):3158-68.



Molecular Weight (MW)

474.55
Formula

C26H30N6O3
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

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

other peoduct :References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/19393476

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.

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