[CAS NO. 1600515-49-8] Tilfrinib

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PRODUCTS SPECIFICATIONS [1600515-49-8]

Catalog

HY-110244

Brand

MCE

CAS

1600515-49-8

DESCRIPTION [1600515-49-8]

Overview

MDL	-
Molecular Weight	275.30
Molecular Formula	C17H13N3O
SMILES	OC1=CC=CC(NC2=C3C4=CC=CC=C4NC3=NC=C2)=C1

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

Summary

Tilfrinib (compound 4f) is a potent and selective Brk/PTK6 inhibitor with an IC ₅₀ value of 3.15 nM for Brk . Tilfrinib shows good anti-proliferative activity and has potential of anti-tumour ^[1] ^[2] .

IC50 & Target

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

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 GI ₅₀ values of 0.99, 1.02 and 1.58 µM ^[2] .

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.

Appearance

Solid

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)

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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

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
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
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

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

* All of the co-solvents are available by MCE.