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  4. GCN2-IN-7

GCN2-IN-7 (compound 39) is an orally active and selective general control nonderepressible 2 (GCN2) inhibitor (IC50=5 nM). GCN2-IN-7 shows anti-tumor activity in vivo.

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

GCN2-IN-7 Chemical Structure

GCN2-IN-7 Chemical Structure

CAS No. : 2396465-33-9

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 1102 In-stock
Solution
10 mM * 1 mL in DMSO USD 1102 In-stock
Solid
1 mg USD 380 In-stock
5 mg USD 950 In-stock
10 mg USD 1600 In-stock
25 mg USD 3350 In-stock
50 mg USD 5350 In-stock
100 mg USD 8450 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

GCN2-IN-7 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GCN2-IN-7 (compound 39) is an orally active and selective general control nonderepressible 2 (GCN2) inhibitor (IC50=5 nM). GCN2-IN-7 shows anti-tumor activity in vivo[1].

IC50 & Target

IC50: 5 nM (GCN2)[1]
In Vitro

GCN2-IN-7 (600 nM; 3 d) alleviates myeloid-derived suppressive cells (MDSC)-related T cell suppression and restores T cell proliferation[1].

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

GCN2-IN-7 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: CD8+ T cells from WT and GCN2KO cells
Concentration: 600 nM
Incubation Time: 3 days
Result: Relieved MDSC suppression of proliferation of the co-cultured CD8+ T cells with significant relief at 600 nM.
In Vivo

GCN2-IN-7 (oral gavage; 15 mg/kg; BID; 17 d) shows robust target engagement in vivo at a reasonable dose[1].
GCN2-IN-7 (oral gavage; 50 mg/kg; BID; 17 d) inhibits tumor growth in vivo of the LL2 syngeneic mouse tumor model[1].

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

Animal Model: Balb/c mice injected with RENCA cells[1]
Dosage: 15 mg/kg
Administration: Oral gavage; 15 mg/kg; BID; 17 days
Result: Showed robust target engagement of GCN2 in both tumor (average of 84%) and spleen (average of 80%) tissues.
Showed an average of 65% reduction of downstream marker Activation Transcription Factor 4 (ATF4) in compound-treated mice compared to the vehicle treatment group.
Animal Model: LL2 syngeneic mouse model[1]
Dosage: 50 mg/kg
Administration: Oral gavage; 50 mg/kg; BID; 17 days
Result: Showed tumor growth inhibition (56%) after 26 days of dosing compared to the vehicle group.
Molecular Weight

527.44

Formula

C22H23BrN8OS
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@@]1(C)C[C@H](NC2=NC=C3C(N(C4=CC=C(C5=NN=C(C)S5)C=C4)N=C3Br)=N2)CC1)NC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

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

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (94.80 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 1.8960 mL 9.4798 mL 18.9595 mL
5 mM 0.3792 mL 1.8960 mL 3.7919 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 and light). 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
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Concentration
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Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.74 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)

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 and light)

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: 99.85%

COA (254 KB) HNMR (277 KB) RP-HPLC (260 KB) MS (69 KB)

Handling Instructions (2659 KB)
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 and light). 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 1.8960 mL 9.4798 mL 18.9595 mL 47.3988 mL
5 mM 0.3792 mL 1.8960 mL 3.7919 mL 9.4798 mL
10 mM 0.1896 mL 0.9480 mL 1.8960 mL 4.7399 mL
15 mM 0.1264 mL 0.6320 mL 1.2640 mL 3.1599 mL
20 mM 0.0948 mL 0.4740 mL 0.9480 mL 2.3699 mL
25 mM 0.0758 mL 0.3792 mL 0.7584 mL 1.8960 mL
30 mM 0.0632 mL 0.3160 mL 0.6320 mL 1.5800 mL
40 mM 0.0474 mL 0.2370 mL 0.4740 mL 1.1850 mL
50 mM 0.0379 mL 0.1896 mL 0.3792 mL 0.9480 mL
60 mM 0.0316 mL 0.1580 mL 0.3160 mL 0.7900 mL
80 mM 0.0237 mL 0.1185 mL 0.2370 mL 0.5925 mL
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GCN2-IN-7 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:

GCN2-IN-72396465-33-9Othersoral activityselectivityanti-tumor activityCD8+ T cellsInhibitorinhibitorinhibit

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