Purdue Bioscience - SpeciPure

E7449 is a potent PARP1 and PARP2 inhibitor and also inhibits TNKS1 and TNKS2, with IC50s of 2.0, 1.0, ～50 and ～50 nM for PARP1, PARP2, TNKS1 and TNKS2, respectively, using 32P-NAD+ as substrate.

Pack Size	Availability	Price/USD
1 mg	In stock	$ 110
2 mg	In stock	$ 198
4 mg	In stock	$ 277
10 mg	In stock	$ 551
20 mg	In stock	$ 881

Description	E7449 is a potent PARP1 and PARP2 inhibitor and also inhibits TNKS1 and TNKS2, with IC50s of 2.0, 1.0, ～50 and ～50 nM for PARP1, PARP2, TNKS1 and TNKS2, respectively, using 32P-NAD+ as substrate.
Targets&IC50	TNKS1:50 nM (IC50), PARP2:1 nM (IC50), PARP1:2 nM (IC50), TNKS2:50 nM (IC50)
In vitro	E7449 shows no obvious inhibiotry effects on PARP3 or PARPs 6-16. E7449 traps PARP1 onto damaged DNA, and affects DNA repair pathways beyond homologous recombination (HR). E7449 most potnetly suppresses cells deficient in components of the HR pathway (BRCA1 and 2, CtIP, Rad54). E7449 (10 μM) inhibits Wnt signaling in SW480 cells.
In vivo	E7449 moderately inhibits the growth of tumors at 100 mg/kg, and significantly ehhances the inhibition via 10, 30 and 100 mg/kg oral dosing in combination with temozolomide (TMZ) in the mouse melanoma B16-F10 isograft model.
Synonyms	UNII-9X5A2QIA7C
CAS No.	1140964-99-3
Chemical Formula	C18H15N5O
Molecular Weight	317.352
Solubility	DMSO: 6.4 mg/mL (20.17 mM), Need ultrasonic and warming DMSO: 6.5mg/mL (20.5 mM)
Storage	Powder: -20°C for 2 years In solvent: -80°C for 1 year

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation ：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please refer to the datasheet of our products for more information about solubility. Some auxiliary solubilization methods such as sonication, heating, and vortex shaking may be able to assist in the dissolution of the product.

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E7449

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