GNE-272

Name: GNE-272
Brand: TargetMol
SKU: T15400
Price: 192 USD
Availability: InStock
Rating: 4.5 (1 reviews)

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产品编号 T15400Cas号 1936428-93-1

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.

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GNE-272

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产品编号 T15400Cas号 1936428-93-1

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.

规格	价格	库存
2 mg	¥ 913	6-8周
5 mg	¥ 1,720	6-8周
25 mg	¥ 7,690	6-8周
50 mg	¥ 9,990	6-8周
100 mg	¥ 15,800	6-8周

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产品介绍

生物活性

产品描述	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.
靶点活性	BRD4:13 μM, CBP:0.02 μM, EP300:0.03 μM
体外活性	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.
体内活性	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.

化学信息

分子量	424.47
分子式	C₂₂H₂₅FN₆O₂
CAS No.	1936428-93-1
密度	1.43 g/cm3 (Predicted)

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

DMSO: 100 mg/mL (235.59 mM), Sonication is recommended.

溶液配制表

	1mg	5mg	10mg	50mg
1 mM	2.3559 mL	11.7794 mL	23.5588 mL	117.7940 mL
5 mM	0.4712 mL	2.3559 mL	4.7118 mL	23.5588 mL
10 mM	0.2356 mL	1.1779 mL	2.3559 mL	11.7794 mL
20 mM	0.1178 mL	0.5890 mL	1.1779 mL	5.8897 mL
50 mM	0.0471 mL	0.2356 mL	0.4712 mL	2.3559 mL
100 mM	0.0236 mL	0.1178 mL	0.2356 mL	1.1779 mL