Purdue Bioscience - SpeciPure

GNE-272 is a selective inhibitor of CBP/EP300 (IC50: 0.02, 0.03, and 13 μM for CBP, EP300, and BRD4, respectively) and a selective in vivo probe for CBP/EP300.

Pack Size	Availability	Price/USD
2 mg	6-8 weeks	$ 158
4 mg	6-8 weeks	$ 284
8 mg	6-8 weeks	$ 480
20 mg	6-8 weeks	$ 873
40 mg	6-8 weeks	$ 1318

Description	GNE-272 is a selective inhibitor of CBP/EP300 (IC50: 0.02, 0.03, and 13 μM for CBP, EP300, and BRD4, respectively) and a selective in vivo probe for CBP/EP300.
Targets&IC50	BRD4:13 μM, CBP:0.02 μM, EP300:0.03 μM
In vitro	GNE-272 does not inhibit any target at >30% when tested at 10 μM in 35 kinase panel and 42 receptors off-target screening panel. GNE-272 does not inhibit (>10 μM, top concentration) several cytochrome P450s (3A4, 1A2, 2C9, 2C19, 2D6). GNE-272 is exquisitely selective for CBP/ EP300 and remarkably selective (650-fold) over BRD4. The compound has good potency in the BRET cellular assay. GNE-272 is shown to inhibit the expression of MYC10 (MV4?11 cell line) (EC50: 0.91 μM) and a good correlation between the BRET and MYC cellular assays is observed.
In vivo	GNE-272 displays a marked antiproliferative effect in hematologic cancer cell lines. Which modulates MYC expression in vivo that corresponds with antitumor activity in an AML tumor model. GNE-272 shows low clearance following a 1 mg/ kg intravenous dose in a mouse PK experiment and good oral bioavailability when dosed at 100 mg/kg, reaching an unbound Cmax of 26 μM.
CAS No.	1936428-93-1
Chemical Formula	C22H25FN6O2
Molecular Weight	424.48
Solubility	DMSO: 100 mg/mL (235.59 mM), Need ultrasonic
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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GNE-272

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