Art. -Nr.: HY-148494

Tivumecirnon

Name: Tivumecirnon
Brand: MedChemExpress
SKU: HY-148494
Price: 520.00 USD
Availability: InStock
Rating: 5 (1 reviews)

(Synonyms: FLX475)

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Based on 1 Customer Validation

Tivumecirnon (FLX475) is an orally active, selective CCR4 antagonist. Tivumecirnon blocks the binding of CCR4 to its ligands, CCL17 and CCL22, thereby reducing Treg infiltration into the tumor microenvironment. Tivumecirnon has antitumor activity.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 99.48%
CAS. Nr.: 2174938-78-2
Formel: C₂₄H₂₇Cl₂F₃N₆O
Molecular Weight:543.41

Speicherung:

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

Tivumecirnon Chemical Structure

CAS. Nr.: 2174938-78-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[2]

CCR4

Alle CCR Isoform-spezifische Produkte anzeigen :

In Vitro

Tivumecirnon is used in combination with Pembrolizumab (HY-P9902) for the treatment of non-small cell lung cancer^[1].

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

Related Protocols :

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2174938-78-2
Appearance Solid
Molecular Weight 543.41
Formel C₂₄H₂₇Cl₂F₃N₆O
Color Off-white to light yellow
SMILES

C[C@H](C1=C(C=C(C=C1)Cl)Cl)N2C3=NC(N4CC([C@H]5CCCN(C5)CCO)C4)=CN=C3C(C(F)(F)F)=N2
Synonyms

FLX475
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (184.02 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

1.8402 mL

9.2012 mL

18.4023 mL

5 mM

0.3680 mL

1.8402 mL

3.6805 mL

10 mM

0.1840 mL

0.9201 mL

1.8402 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 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. Tae Min Kim, et al. 629-C Phase 2 safety and efficacy of oral CCR4 antagonist FLX475 (tivumecirnon) plus pembrolizumab in subjects with non-small cell lung cancer not previously treated with checkpoint inhibitor[J]. 2023.

[2]. Hilary Plake BECK, et al. Chemokine receptor modulators and uses thereof. WO2018022992.

[3]. Adam Grant, et al. Abstract 2485: A combined mregDC and Treg signature associates with antitumor efficacy of CCR4 antagonist tivumecirnon FLX475. Cancer Res 15 March 2024; 84 (6_Supplement): 2485.

[4]. Dirk G. Brockstedt, et al., Clinical and biological activity of FLX475, an oral CCR4 antagonist, in advanced cancer. Journal of Clinical Oncology. 2023. 41, 2625-2625.

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	1.8402 mL	9.2012 mL	18.4023 mL	46.0058 mL
	5 mM	0.3680 mL	1.8402 mL	3.6805 mL	9.2012 mL
	10 mM	0.1840 mL	0.9201 mL	1.8402 mL	4.6006 mL
	15 mM	0.1227 mL	0.6134 mL	1.2268 mL	3.0671 mL
	20 mM	0.0920 mL	0.4601 mL	0.9201 mL	2.3003 mL
	25 mM	0.0736 mL	0.3680 mL	0.7361 mL	1.8402 mL
	30 mM	0.0613 mL	0.3067 mL	0.6134 mL	1.5335 mL
	40 mM	0.0460 mL	0.2300 mL	0.4601 mL	1.1501 mL
	50 mM	0.0368 mL	0.1840 mL	0.3680 mL	0.9201 mL
	60 mM	0.0307 mL	0.1534 mL	0.3067 mL	0.7668 mL
	80 mM	0.0230 mL	0.1150 mL	0.2300 mL	0.5751 mL
	100 mM	0.0184 mL	0.0920 mL	0.1840 mL	0.4601 mL

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Tivumecirnon

Alle CCR Isoform-spezifische Produkte anzeigen