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UM-164 Src inhibitor

Name: UM-164
SKU: S8706
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.S8706

UM-164 is a highly potent, dual c-Src/p38inhibitor of c-Src with a binding constant Kd of 2.7 nM for c-Src and this compound inhibits both p38α and p38β.

Chemical Structure

Molecular Weight: 640.68

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S870601 DMSO]100 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.12%

99.12

Related Targets	EGFR VEGFR PDGFR FGFR c-Met FLT3 HER2 c-Kit Bcr-Abl MEK BTK IGF-1R ALK Trk receptor Syk Axl CSF-1R c-RET FAK Mertk Tie-2 DYRK Tyro3 Ephrin receptor ROS1 Pyk2 RON DDR ACK Fer kinase
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Chemical Information, Storage & Stability

Molecular Weight	640.68	Formula	C₃₀H₃₁F₃N₈O₃S	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	903564-48-7	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=C(C=C(C=C1)NC(=O)C2=CC(=CC=C2)C(F)(F)F)NC(=O)C3=CN=C(S3)NC4=CC(=NC(=N4)C)N5CCN(CC5)CCO

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (156.08 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.700mg/ml (1.09mM)	Taking the 1 mL working solution as an example, add 50 μL of 14 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMS0 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (7.80mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	p38α ^[1] p38β ^[1] c-Src ^[1] (Cell-free assay) 2.7 nM(Kd)
In vitro	UM-164 binds the inactive kinase conformation of c-Src. This compound alters the cell localization of c-Src in TNBC (anti-triple-negative breast cancer) cells. It has potent antiproliferative activity (average GI50 = 160 nmol/L) in all TNBC cell lines tested. This chemical is a potent inhibitor of p38α and p38β. p38 MAPK phosphorylation is completely absent in SUM 149 cells treated with 50 nmol/L of this compound. It can suppress both cell motility and invasion of MDA-MB 231 and SUM 149 cell lines with an IC50 = 50 nmol/L. FAK phosphorylation is inhibited by this chemical in SUM 149 cells. It also efficiently reduces activation of EGFR (at both Tyr-845 and Tyr-1068), AKT, and ERK1/2, all of which are not direct targets of this compound.^[1].
In vivo	In xenograft models of TNBC (anti-triple-negative breast cancer), UM-164 results in a significant decrease of tumor growth compared with controls, with limited in vivo toxicity^[1].
References	[1] https://pubmed.ncbi.nlm.nih.gov/27154914/

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