Danusertib (PHA-739358)

Catalog No. A10715

Danusertib (PHA-739358)是Aurora A/B/C的Aurora激酶抑制剂，在无细胞分析中的IC50为13 nM/79nM/61 nM，对Abl，TrkA，c-RET和FGFR1以及更低的浓度具有中等效力对Lck，VEGFR2/3，c-Kit，CDK2等有效。

Product Citations

Samuel Q. Li, etc. Targeting Wild-Type and Mutationally Activated FGFR4 in Rhabdomyosarcoma with the Inhibitor Ponatinib (AP24534). PLoS One. 2013; 8(10): e76551.

Technical details

Catalog Num	A10715
M. Wt	474.6
Formula	C26H30N6O3
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	827318-97-8
Synonyms	PHA739358
SMILES	CN1CCN(CC1)C2=CC=C(C=C2)C(=O)NC3=NNC4=C3CN(C4)C(=O)[C@@H](C5=CC=CC=C5)OC

Biological Activity

Targets

Target	Value
AuroraA	IC50: 13nM
Abl	IC50: 25nM
RET	IC50: 31nM
TrkA	IC50: 31nM
FGFR1	IC50: 47nM
AuroraC	IC50: 61nM
AuroraB	IC50: 79nM

Solubility *

In vitro (25°C)	DMSO	93 mg/mL (195.97 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	1% DMSO+30% polyethylene glycol+1% Tween 80	28 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	21.07 mL	105.35 mL	210.7 mL
0.5 mM	4.21 mL	21.07 mL	42.14 mL
1 mM	2.11 mL	10.54 mL	21.07 mL
5 mM	0.42 mL	2.11 mL	4.21 mL

*The above data is based on the productmolecular weight 474.6 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.