Tilfrinib

Name: Tilfrinib
Brand: MedChemExpress
SKU: HY-110244
Rating: 4.5 (1 reviews)

Cat. No.: HY-110244 Purity: 99.69%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

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

Tilfrinib Chemical Structure

CAS No. : 1600515-49-8

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 121	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 121	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 170	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 590	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 950	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity
Purity & Documentation
References
Customer Review

Description

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.

Molecular Weight

275.30

Formula

C₁₇H₁₃N₃O

CAS No.

1600515-49-8

Appearance

Solid

Color

Off-white to yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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. 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 2.08 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

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).

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: 99.69%

Select Batch:

Data Sheet (279 KB) SDS (251 KB)

COA (255 KB) LCMS (94 KB) Elemental Analysis Report (113 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

Tilfrinib 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:

Tilfrinib1600515-49-8BRKBreast tumor kinaseProtein tyrosine kinase 6 (PTK6)anti-tumouranti-proliferationcancerUM-UC-3MCF7HS-578/TBT-549Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

Tilfrinib

Customer Review

Tilfrinib Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

Tilfrinib Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Tilfrinib Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report