Cat. No.: HY-160215

GFH018

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GFH018 is an orally active, selective and ATP-competitive TGF-βR1 inhibitor with an IC₅₀ of 40 nM. GFH018 reactivates the immune system by blocking the immunosuppression mediated by regulatory T cells and M2 macrophages. GFH018 inhibits tumor angiogenesis. GFH018 suppresses tumor growth in mouse tumor models. GFH018 can be used for the research of solid tumors, hepatocellular carcinoma, colorectal cancer, breast cancer, and relapsed/metastatic nasopharyngeal carcinoma.

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

Purity: 98.59%
CAS No.: 2169299-67-4
Formula: C₂₁H₁₉N₇O
Molecular Weight:385.42

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

GFH018 Chemical Structure

CAS No.: 2169299-67-4

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

IL-6

IL-10

All TGF-β Receptor Isoforms :

All p38 MAPK Isoforms :

All TGF-beta/Smad Isoforms :

Smad1
Smad3

All Interleukin Related Isoforms :

In Vitro

GFH018 (0.2 nM-40 μM; 40 min) inhibits p38α enzymatic activity with an IC₅₀ of 2,648 nM, and is 66.2-fold more selective for TGF-βR1 than for p38α^[1].
GFH018 inhibits the proliferation of NIH 3T3 fibroblasts with an IC₅₀ of 0.73 μM^[1].
GFH018 inhibits TGF-β-induced Smad phosphorylation in HEK293 reporter cells, with an IC₅₀ of 105 nM^[1].
GFH018 (0.1-10 μM; 4 days) dose-dependently inhibits TGF-β-induced Treg differentiation in a mouse CD4⁺ T cell-APC co-culture system, with the strongest inhibitory effect observed at the concentration of 10 μM^[1].
GFH018 (0.1-10 μM; 16 h) regulates cytokine secretion in human M2 macrophages in a dose-dependent manner, upregulating TNF-α and IL-6 levels while downregulating IL-10 levels at concentrations ranging from 0.1 to 10 μM^[1].
GFH018 (0.1-10 μM; 6 h) inhibits tube formation of HUVEC cells on Matrigel in a dose-dependent manner. After 6 h of incubation, significant reductions in the number of nodes and tube length are observed at concentrations ranging from 0.1 to 10 μM^[1].

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

Parmacokinetics

Species	Dose	Route	T_1/2	V_dss	CL	AUC_0-last	C_max	Bioavailability
Mice^[1]	1 mg/kg	i.v.	0.484 h	1.4 L/kg	63.3 mL/min/kg	/	/	/
Mice^[1]	5 mg/kg	p.o.	0.917 h	/	/	285 nM·h/mL	355 nM/mL	8.74 %
Mice^[1]	75 mg/kg	p.o.	0.856 h	/	/	18137 nM·h/mL	24233 nM/mL	36.8 %
Rat^[1]	1 mg/kg	i.v.	0.87 h	1.44 L/kg	33.3 mL/min/kg	1332 nM·h/mL	/	/
Rat^[1]	30 mg/kg	p.o.	2.01 h	/	/	9614 nM·h/mL	9553 nM/mL	29.9 %
Dog^[1]	1 mg/kg	i.v.	3.16 h	0.961 L/kg	9.29 mL/min/kg	5626 nM·h/mL	/	/
Dog^[1]	5 mg/kg	p.o.	2.83 h	/	/	18284 nM·h/mL	5633 nM/mL	65.5 %

In Vivo

GFH018 (15-50 mg/kg; p.o.; twice daily; for 11 consecutive days) exhibits dose-dependent in vivo anti-tumor activity in a mouse liver cancer model^[1].
GFH018 (50 mg/kg; p.o.; twice daily) and anti-PD-L1 antibody exerts synergistic antitumor efficacy in a mouse colorectal cancer model, with a TGI of 79.4%^[1].
GFH018 (100 mg/kg; p.o.; twice daily; for 32 days) potently inhibits the metastasis of breast cancer to multiple organs in vivo at an oral dose of 100 mg/kg twice daily^[1].

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

Animal Model:

BALB/c (female, 6-8 weeks old, subcutaneous inoculation of H22 murine hepatocellular carcinoma cells)^[1]
Dosage:

15 mg/kg; 50 mg/kg
Administration:

p.o.; twice daily; 11 days
Result:

Induced tumor growth delay in a dose-dependent manner, with tumor growth inhibition (TGI) of 50.8% at 15 mg/kg and 57.5% at 50 mg/kg.
Sustained plasma exposure covering the in vitro p-Smad IC₅₀ for approximately 3.5 h after the last 15 mg/kg dose and 5.5 h after the last 50 mg/kg dose.
Significantly reduced phosphorylated Smad3 protein levels in H22 tumors compared to vehicle control at 1 h post-final dose; inhibition was nearly absent at 12 h post-dose.

Chemical Information

CAS No. 2169299-67-4
Appearance Solid
Molecular Weight 385.42
Formula C₂₁H₁₉N₇O
Color White to off-white
SMILES

NC(/C=C/C1=C(C=CC2=NC=NN21)C3=C(CCC4)N4N=C3C5=CC=CC(C)=N5)=O
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (259.46 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5946 mL

12.9729 mL

25.9457 mL

5 mM

0.5189 mL

2.5946 mL

5.1891 mL

10 mM

0.2595 mL

1.2973 mL

2.5946 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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: ≥ 5 mg/mL (12.97 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 5 mg/mL (12.97 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (12.97 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Jiang T, et al. Discovery of a Selective, Novel TGF-βR1 Inhibitor GFH018 for the Treatment of Solid Tumors. J Med Chem. 2025;68(12):12513-12530. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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	2.5946 mL	12.9729 mL	25.9457 mL	64.8643 mL
	5 mM	0.5189 mL	2.5946 mL	5.1891 mL	12.9729 mL
	10 mM	0.2595 mL	1.2973 mL	2.5946 mL	6.4864 mL
	15 mM	0.1730 mL	0.8649 mL	1.7297 mL	4.3243 mL
	20 mM	0.1297 mL	0.6486 mL	1.2973 mL	3.2432 mL
	25 mM	0.1038 mL	0.5189 mL	1.0378 mL	2.5946 mL
	30 mM	0.0865 mL	0.4324 mL	0.8649 mL	2.1621 mL
	40 mM	0.0649 mL	0.3243 mL	0.6486 mL	1.6216 mL
	50 mM	0.0519 mL	0.2595 mL	0.5189 mL	1.2973 mL
	60 mM	0.0432 mL	0.2162 mL	0.4324 mL	1.0811 mL
	80 mM	0.0324 mL	0.1622 mL	0.3243 mL	0.8108 mL
	100 mM	0.0259 mL	0.1297 mL	0.2595 mL	0.6486 mL

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GFH018

Bioactive Compound Library Max

Bioactive Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Stem Cell Signaling Compound Library

TGF-beta/Smad Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Covalent Screening Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Pyroptosis Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Transcription Factor-Targeted Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Antidepressant Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Osteogenesis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Ovarian Cancer Compound Library

Macrophage Related Compound Library

Multi-Target Compound Library

MCE Bioactive Compound Library

Covalent Screening Library Plus

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Lactylation Compound Library

All TGF-β Receptor Isoforms

All p38 MAPK Isoforms

All TGF-beta/Smad Isoforms

All Interleukin Related Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

GFH018 Related Classifications

HY-160215 Related Classifications