GNE-272

Name: GNE-272
Brand: MedChemExpress
SKU: HY-100726
Rating: 5.0 (3 reviews)

Cat. No.: HY-100726 Purity: 99.76%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

GNE-272 is a potent and selective CBP/EP300 inhibitor with IC₅₀ values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. GNE-272 is also a selective in vivo probe for CBP/EP300.

For research use only. We do not sell to patients.

GNE-272 Chemical Structure

CAS No. : 1936428-93-1

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 213	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 213	In-stock	Estimated Time of Arrival: December 31
Solid
2 mg	USD 132	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 228	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 360	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1140	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1800	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 3 publication(s) in Google Scholar

2 Publications Citing Use of MCE GNE-272

: GNE-272 purchased from MedChemExpress. Usage Cited in: J Transl Med. 2023 Mar 17;21(1):201. [Abstract]; GNE-272 downregulates the expression of SNAI2 both in BxPC-3 and PANC1.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

CBP/p300

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	410 nM Compound: 1; GNE-272	Inhibition of Halo-tagged histone H3.3 binding to NanoLuc luciferase conjugated human CBP expressed in HEK293 cells after overnight incubation by BRET assay Inhibition of Halo-tagged histone H3.3 binding to NanoLuc luciferase conjugated human CBP expressed in HEK293 cells after overnight incubation by BRET assay	[PMID: 28892380]
MV4-11	EC₅₀	1.9 μM Compound: ent-59	Inhibition of CBP/EP300 in human MV4-11 cells assessed as inhibition of MYC expression measured after 4 hrs by luminescence analysis Inhibition of CBP/EP300 in human MV4-11 cells assessed as inhibition of MYC expression measured after 4 hrs by luminescence analysis	[PMID: 27682507]

In Vitro

GNE-272 is exquisitely selective for CBP/ EP300 and remarkably selective (650-fold) over BRD4. When tested at 10 μM in 35 kinase panel and 42 receptors off-target screening panel, GNE-272 does not inhibit any target at >30%. In addition, GNE-272 does not inhibit (>10 μM, top concentration) several cytochrome P450s (3A4, 1A2, 2C9, 2C19, 2D6). The compound has good potency in the BRET cellular assay. In an orthogonal measure of the target engagement, GNE-272 is shown to inhibit the expression of MYC10 (MV4?11 cell line) with an EC₅₀ of 0.91 μM and good correlation between the BRET and MYC cellular assays is observed^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

GNE-272 demonstrates 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 C_max of 26 μM. GNE-272 shows a marked antiproliferative effect in hematologic cancer cell lines and modulates MYC expression in vivo that corresponds with antitumor activity in an AML tumor model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

424.47

Formula

C₂₂H₂₅FN₆O₂

CAS No.

1936428-93-1

Appearance

Solid

Color

White to off-white

SMILES

CC(N1CCC2=C(C(NC3=C(F)C=C(C4=CN(C)N=C4)C=C3)=NN2[C@@H]5COCC5)C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (235.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3559 mL	11.7794 mL	23.5588 mL
5 mM	0.4712 mL	2.3559 mL	4.7118 mL
10 mM	0.2356 mL	1.1779 mL	2.3559 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.89 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.89 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.89 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.76%

Select Batch:

Data Sheet (277 KB) SDS (251 KB)

COA (251 KB) LCMS (266 KB)

Handling Instructions (2659 KB)

References

[1]. Crawford TD, et al. Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300. J Med Chem. 2016 Dec 8;59(23):10549-10563. [Content Brief]

Cell Assay ^[1]	Human cancer cell lines (MOLM-16, HL-60, LP-1, KMS-34, Pfeiffer, DOHH-2) are treated for 4 h with 5 μM GNE-272 or DMSO control. After 6 days, cell viability is measured by CellTiter-Glo^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice: Mice are given 0 (vehicle, 0.5% methylcellulose; 0.2% Tween-80), 12.5, 25, and 50 mg/kg of GNE-272 by gavage, twice daily (BID) for 21 days in a volume of 100 μL. Tumor volumes are measured in two dimensions (length and width) using Ultra CalIV calipers and analyzed using Excel, version 11.2^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Crawford TD, et al. Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300. J Med Chem. 2016 Dec 8;59(23):10549-10563. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3559 mL	11.7794 mL	23.5588 mL	58.8970 mL
	5 mM	0.4712 mL	2.3559 mL	4.7118 mL	11.7794 mL
	10 mM	0.2356 mL	1.1779 mL	2.3559 mL	5.8897 mL
	15 mM	0.1571 mL	0.7853 mL	1.5706 mL	3.9265 mL
	20 mM	0.1178 mL	0.5890 mL	1.1779 mL	2.9448 mL
	25 mM	0.0942 mL	0.4712 mL	0.9424 mL	2.3559 mL
	30 mM	0.0785 mL	0.3926 mL	0.7853 mL	1.9632 mL
	40 mM	0.0589 mL	0.2945 mL	0.5890 mL	1.4724 mL
	50 mM	0.0471 mL	0.2356 mL	0.4712 mL	1.1779 mL
	60 mM	0.0393 mL	0.1963 mL	0.3926 mL	0.9816 mL
	80 mM	0.0294 mL	0.1472 mL	0.2945 mL	0.7362 mL
	100 mM	0.0236 mL	0.1178 mL	0.2356 mL	0.5890 mL

GNE-272 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GNE-2721936428-93-1GNE272GNE 272Histone AcetyltransferaseEpigenetic Reader DomainHATsHATInhibitorinhibitorinhibit

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GNE-272

Customer Review

GNE-272 Related Antibodies

2 Publications Citing Use of MCE GNE-272

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References

Customer Review

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Complete Stock Solution Preparation Table

GNE-272 Related Classifications

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