2. GPCR/G Protein Immunology/Inflammation
  3. CCR
  4. Tivumecirnon

Tivumecirnon  (Synonyms: FLX475)

Cat. No.: HY-148494 Purity: 99.85%
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Tivumecirnon (FLX475) is an orally bioactive, selective CCR4 antagonist. Tivumecirnon can block the recruitment of immunosuppressive regulatory T cells (Treg) into the tumor microenvironment, leading to enhanced antitumor activity. Tivumecirnon has antitumor activity on EBV+ NK/T cell lymphoma and non-small cell lung cancer (NSCLC) combined with Pembrolizumab (HY-P9902). Tivumecirnon is promising for research of broad range of tumor types.

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

Tivumecirnon Chemical Structure

Tivumecirnon Chemical Structure

CAS No. : 2174938-78-2

Size Price Stock Quantity
5 mg USD 610 In-stock
10 mg USD 980 In-stock
25 mg USD 2020 In-stock
50 mg USD 3250 In-stock
100 mg USD 5250 In-stock
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Based on 1 publication(s) in Google Scholar

Tivumecirnon Related Antibodies

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CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

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Description

Tivumecirnon (FLX475) is an orally bioactive, selective CCR4 antagonist. Tivumecirnon can block the recruitment of immunosuppressive regulatory T cells (Treg) into the tumor microenvironment, leading to enhanced antitumor activity. Tivumecirnon has antitumor activity on EBV+ NK/T cell lymphoma and non-small cell lung cancer (NSCLC) combined with Pembrolizumab (HY-P9902). Tivumecirnon is promising for research of broad range of tumor types[1][2][3][4].
IC50 & Target[2]

CCR4

 

Clinical Trial
Molecular Weight

543.41

Formula

C24H27Cl2F3N6O
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8402 mL 9.2012 mL 18.4023 mL
5 mM 0.3680 mL 1.8402 mL 3.6805 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.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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    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

mg/kg

Animal weight
(per animal)

g

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
References

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.

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 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:

Tivumecirnon2174938-78-2FLX475FLX 475FLX-475CCRCC chemokine receptorCCR4 antagonistregulatory T celltumor microenvironmentantitumor activityEBV+ NK/T cell lymphomanon-small cell lung cancer (NSCLC)Inhibitorinhibitorinhibit

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