Art. -Nr.: HY-110244

Tilfrinib

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Tilfrinib (compound 4f) is a potent and selective Brk/PTK6 inhibitor with an IC₅₀ value of 3.15 nM for Brk. Tilfrinib shows good anti-proliferative activity and has potential of anti-tumour.

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Reinheit: 99.39%
CAS. Nr.: 1600515-49-8
Formel: C₁₇H₁₃N₃O
Molecular Weight:275.30

Speicherung:

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

Tilfrinib Chemical Structure

CAS. Nr.: 1600515-49-8

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 3.15 nM (Brk), PTK6^[1]^[2].

Cellular Effect

Cell Line	Type	Value	Description	References
BT-549	GI₅₀	1.58 μM Compound: 4f	Antiproliferative activity against human BT549 cells by sulfur rhodamine assay Antiproliferative activity against human BT549 cells by sulfur rhodamine assay	[PMID: 24650640]
Hs-578T	GI₅₀	1.02 μM Compound: 4f	Antiproliferative activity against human Hs 578T cells by sulfur rhodamine assay Antiproliferative activity against human Hs 578T cells by sulfur rhodamine assay	[PMID: 24650640]
MCF7	GI₅₀	0.89 μM Compound: 5b	Antiproliferative activity against human MCF7 cells by SRB assay Antiproliferative activity against human MCF7 cells by SRB assay	10.1039/C4MD00028E
MCF7	GI₅₀	0.99 μM Compound: 4f	Antiproliferative activity against human MCF7 cells by sulfur rhodamine assay Antiproliferative activity against human MCF7 cells by sulfur rhodamine assay	[PMID: 24650640]
MDA-MB-468	GI₅₀	1 μM Compound: 5b	Antiproliferative activity against human MDA-MB-468 cells by SRB assay Antiproliferative activity against human MDA-MB-468 cells by SRB assay	10.1039/C4MD00028E
Sf9	IC₅₀	1300 nM Compound: 5b	Inhibition of human recombinant GST-fused HER2 expressed in baculovirus Sf9 insect cells using poly(Glu,Tyr) as substrate after 60 mins by scintillation counting Inhibition of human recombinant GST-fused HER2 expressed in baculovirus Sf9 insect cells using poly(Glu,Tyr) as substrate after 60 mins by scintillation counting	10.1039/C4MD00028E
Sf9	IC₅₀	3.2 nM Compound: 5b	Inhibition of human recombinant GST-fused Brk expressed in baculovirus Sf9 insect cells using poly(Glu,Tyr) as substrate after 60 mins by scintillation counting Inhibition of human recombinant GST-fused Brk expressed in baculovirus Sf9 insect cells using poly(Glu,Tyr) as substrate after 60 mins by scintillation counting	10.1039/C4MD00028E

In Vitro

Tilfrinib (20 μM; 36 h) shows inhibition of PTK6, and decreases the ETV4 WT-induced expression of CXCL1 or CXCL8 in UM-UC-3 cells and expression of VEGFA or MMP9 in TANs^[1].
Tilfrinib (compound 4f) shows good anti-proliferative activity against MCF7, HS-578/T and BT-549 cells with GI₅₀ values of 0.99, 1.02 and 1.58 μM^[2].

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

Western Blot Analysis^[1]

Cell Line:

UM-UC-3 cells (stably expressing FLAG-ETV4 WT or Y392F)
Concentration:

20 µM
Incubation Time:

36 h
Result:

Reduced ETV4 WT-induced expression of CXCL1 or CXCL8 in UM-UC-3 cells and expression of VEGFA or MMP9 in TANs by inhibiting PTK6.

Chemical Information

CAS. Nr. 1600515-49-8
Appearance Solid
Molecular Weight 275.30
Formel C₁₇H₁₃N₃O
Color Off-white to yellow
SMILES

OC1=CC=CC(NC2=C3C4=CC=CC=C4NC3=NC=C2)=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 125 mg/mL (454.05 mM; Need ultrasonic; 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

3.6324 mL

18.1620 mL

36.3240 mL

5 mM

0.7265 mL

3.6324 mL

7.2648 mL

10 mM

0.3632 mL

1.8162 mL

3.6324 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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: ≥ 2.08 mg/mL (7.56 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (7.56 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (7.56 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 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)

Verweise

[1]. Zhang Q, Liu S, et al. ETV4 mediated tumor-associated neutrophil recruitment promotes lymphangiogenesis and lymphatic metastasis of bladder cancer[J]. 2022.

[2]. Mahmoud KA, et al. Discovery of 4-anilino α-carbolines as novel Brk inhibitors. Bioorg Med Chem Lett. 2014 Apr 15;24(8):1948-51. [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	3.6324 mL	18.1620 mL	36.3240 mL	90.8100 mL
	5 mM	0.7265 mL	3.6324 mL	7.2648 mL	18.1620 mL
	10 mM	0.3632 mL	1.8162 mL	3.6324 mL	9.0810 mL
	15 mM	0.2422 mL	1.2108 mL	2.4216 mL	6.0540 mL
	20 mM	0.1816 mL	0.9081 mL	1.8162 mL	4.5405 mL
	25 mM	0.1453 mL	0.7265 mL	1.4530 mL	3.6324 mL
	30 mM	0.1211 mL	0.6054 mL	1.2108 mL	3.0270 mL
	40 mM	0.0908 mL	0.4541 mL	0.9081 mL	2.2703 mL
	50 mM	0.0726 mL	0.3632 mL	0.7265 mL	1.8162 mL
	60 mM	0.0605 mL	0.3027 mL	0.6054 mL	1.5135 mL
	80 mM	0.0454 mL	0.2270 mL	0.4541 mL	1.1351 mL
	100 mM	0.0363 mL	0.1816 mL	0.3632 mL	0.9081 mL

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Tilfrinib

Kinase Inhibitor Library

Anti-Cancer Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Tilfrinib

Kinase Inhibitor Library

Anti-Cancer Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Tilfrinib Related Classifications

HY-110244 Related Classifications