GNE-272
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 100mg | $1600 | Check With Us |
| 250mg | $2500 | Check With Us |
| 500mg | $3750 | Check With Us |
: Cat #: V4552 CAS #: 1936428-93-1 Purity ≥ 98%
Description: GNE-272 is a novel, potent and selective in vivo chemical probe for and inhibitor of the CBP/EP300 bromodomains with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively.
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- Physicochemical and Storage Information
- Protocol
- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 424.47 |
|---|---|
| Molecular Formula | C22H25FN6O2 |
| CAS No. | 1936428-93-1 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| SMILES Code | CC(N1CCC2=C(C(NC3=C(F)C=C(C4=CN(C)N=C4)C=C3)=NN2[C@H]5CCOC5)C1)=O |
| Synonyms | GNE-272; GNE 272; GNE272. |
| Protocol | 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. |
|---|---|---|
| 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 Cmax 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. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.3559 mL | 11.7794 mL | 23.5588 mL | 47.1176 mL |
| 5mM | 0.4712 mL | 2.3559 mL | 4.7118 mL | 9.4235 mL |
| 10mM | 0.2356 mL | 1.1779 mL | 2.3559 mL | 4.7118 mL |
| 20mM | 0.1178 mL | 0.5890 mL | 1.1779 mL | 2.3559 mL |
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
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Volume
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Molecular Weight*
The dilution calculator equation
Concentration(start)
×
Volume(start)
=
Concentration(final)
×
Volume(final)
This equation is commonly abbreviated as: C1 V1 = C2 V2
Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg
Average weight of animals g
Dosing volume per animal µL
Number of animals
Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
mg/ml;
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.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.