2. Cell Cycle/DNA Damage Apoptosis
  3. Checkpoint Kinase (Chk) Apoptosis
  4. GNE-900

GNE-900 is a an ATP-competitive, selective, and orally active ChK1 inhibitor with IC50s of 0.0011, 1.5 µM for ChKl, ChK2, respectively. GNE-900 abrogates the G2-M checkpoint, enhances DNA damage, and induces Apoptosis. gemcitabine (HY-17026) and GNE-900 administration shows anti-tumor activity.

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

GNE-900 Chemical Structure

GNE-900 Chemical Structure

CAS No. : 1200126-26-6

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Based on 1 publication(s) in Google Scholar

GNE-900 Related Antibodies

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Description

GNE-900 is a an ATP-competitive, selective, and orally active ChK1 inhibitor with IC50s of 0.0011, 1.5 µM for ChKl, ChK2, respectively. GNE-900 abrogates the G2-M checkpoint, enhances DNA damage, and induces Apoptosis. gemcitabine (HY-17026) and GNE-900 administration shows anti-tumor activity[1].

IC50 & Target[1]

Chk1

0.0011 μM (IC50)

Chk2

1.5 μM (IC50)

In Vitro

GNE-900 (1 µM; 1-48 h) induces apoptosis with increases in the expression of cleaved PARP when combined with gemcitabine (50 nM) in HT-29 cells[1].

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

GNE-900 Related Antibodies

Apoptosis Analysis[1]

Cell Line: HT-29 cells
Concentration: 1 µM
Incubation Time: 1-48 h
Result: Inducesd apoptosis with increased the expression of cleaved PARP when combination with gemcitabine (50 nM).
In Vivo

GNE-900 (2.5-40 mg/kg; p.o.; once) decreases the tumor volume and increases DNA damage, γ-H2AX levels when combinated with gemcitabine (HY-17026) in rats[1].

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

Animal Model: Sprague-Dawley rats (HT-29 tumor xenografts)[1]
Dosage: 2.5-40 mg/kg (received a dose of gemcitabine 120 mg/kg)
Administration: P.o.; once
Result: Decreased the tumor volume and resulted in significant enhancement of DNA damage, increased γ-H2AX levels.
Molecular Weight

367.45

Formula

C23H21N5
CAS No.
Appearance

Solid

Color

Light yellow to brown

SMILES

N#CC1=NC=C2C(C3=CC(C4=CC=C(CN5CCCCC5)C=C4)=CN=C3N2)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (272.15 mM; ultrasonic and warming and heat to 80°C; 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 2.7215 mL 13.6073 mL 27.2146 mL
5 mM 0.5443 mL 2.7215 mL 5.4429 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 (6.80 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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
References

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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7215 mL 13.6073 mL 27.2146 mL 68.0365 mL
5 mM 0.5443 mL 2.7215 mL 5.4429 mL 13.6073 mL
10 mM 0.2721 mL 1.3607 mL 2.7215 mL 6.8036 mL
15 mM 0.1814 mL 0.9072 mL 1.8143 mL 4.5358 mL
20 mM 0.1361 mL 0.6804 mL 1.3607 mL 3.4018 mL
25 mM 0.1089 mL 0.5443 mL 1.0886 mL 2.7215 mL
30 mM 0.0907 mL 0.4536 mL 0.9072 mL 2.2679 mL
40 mM 0.0680 mL 0.3402 mL 0.6804 mL 1.7009 mL
50 mM 0.0544 mL 0.2721 mL 0.5443 mL 1.3607 mL
60 mM 0.0454 mL 0.2268 mL 0.4536 mL 1.1339 mL
80 mM 0.0340 mL 0.1701 mL 0.3402 mL 0.8505 mL
100 mM 0.0272 mL 0.1361 mL 0.2721 mL 0.6804 mL
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GNE-900 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-9001200126-26-6GNE900GNE 900Checkpoint Kinase (Chk)Apoptosisorally activeG2-M checkpoint DNA damageapoptosisgemcitabinecleaved PARPHT-29 cellsInhibitorinhibitorinhibit

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