2. Protein Tyrosine Kinase/RTK
  3. Anaplastic lymphoma kinase (ALK) VEGFR
  4. Tosposertib

Tosposertib  (Synonyms: TU2218 free base)

Cat. No.: HY-172240 Purity: 99.89%
COA
SDS
Handling Instructions Technical Support

Tosposertib (TU2218 free base) is an ALK5/VEGFR2 dual inhibitor (IC50 = 1.2 nM/4.9 nM). Tosposertib directly restores the activity of damaged cytotoxic T lymphocytes (CTLs) and natural killer cells inhibited by TGFβ and suppresses the activity and viability of regulatory T cells. Tosposertib can be used for the study of melanoma and colon cancer.

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

Tosposertib

Tosposertib Chemical Structure

CAS No. : 1418305-55-1

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Based on 1 publication(s) in Google Scholar

Tosposertib Related Antibodies

Top Publications Citing Use of Products

View All VEGFR Isoform Specific Products:

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Tosposertib (TU2218 free base) is an ALK5/VEGFR2 dual inhibitor (IC50 = 1.2 nM/4.9 nM). Tosposertib directly restores the activity of damaged cytotoxic T lymphocytes (CTLs) and natural killer cells inhibited by TGFβ and suppresses the activity and viability of regulatory T cells. Tosposertib can be used for the study of melanoma and colon cancer[1].

IC50 & Target[1]

ALK5

1.2 nM (IC50)

VEGFR2

4.9 nM (IC50)

In Vitro

Tosposertib (TU2218) shows a half maximal inhibitory concentration (IC50) of 101 nM in the SMAD2 phosphorylation assay using human whole blood and an IC50 of 52.5 nM in the VEGFR2 phosphorylation assay in human umbilical vein endothelial cells (HUVECs)[1].
Tosposertib (0.5-5 μM, 24 h) can reverse the TGFβ-mediated inhibition of IFNγ expression in CD4+ and CD8+ T cells in human peripheral blood mononuclear cells (PBMCs)[1].
Tosposertib (0.5-5 μM, 72 h) significantly restores TGFβ-induced inhibition of IFNγ secretion in Human PBMCs cells[1].
Tosposertib (0.2-5 μM) upregulates the expression of NKG2D receptor, is inhibited by TGFβ, and restores the killing activity of NK92 cells against K562 cells[1].
Tosposertib (0.5-5 μM, 48 h) can restore the decreased IFNγ level caused by co-culturing Human PBMCs with MCF-7 or HT-1080 cancer cells[1].
Tosposertib (0.5-2.5 μM, 5 days) concentration-dependently restores regulator T cell (Treg)-inhibited effector T cell (Teff) proliferation and reduces Treg activity[1].
Tosposertib upregulates the expression of adhesion-related genes (such as VCAM-1 and ICAM-1) in HUVECs stimulated by TNFα and VEGF, and downregulates cell division-related genes[1].

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

Tosposertib Related Antibodies
In Vivo

Tosposertib (TU2218) enhances the anti-tumor effect of immune checkpoint inhibitors by dually inhibiting ALK5/VEGFR2, and inhibits tumor growth in B16F10, CT26, and WEHI-164 xenograft mouse models[1].

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

317.35

Formula

C17H15N7
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

CC1=CC=CC(C(NC2=NCCN23)=C3C4=CN5N=CN=C5C=C4)=N1
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 (315.11 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 3.1511 mL 15.7555 mL 31.5110 mL
5 mM 0.6302 mL 3.1511 mL 6.3022 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)

Mass
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Concentration
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Volume
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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

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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.88 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (7.88 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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

Purity: 99.89%

SDS (251 KB)

COA (259 KB) HNMR (142 KB) RP-HPLC (162 KB) LCMS (105 KB)

Handling Instructions (2659 KB)
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 3.1511 mL 15.7555 mL 31.5109 mL 78.7774 mL
5 mM 0.6302 mL 3.1511 mL 6.3022 mL 15.7555 mL
10 mM 0.3151 mL 1.5755 mL 3.1511 mL 7.8777 mL
15 mM 0.2101 mL 1.0504 mL 2.1007 mL 5.2518 mL
20 mM 0.1576 mL 0.7878 mL 1.5755 mL 3.9389 mL
25 mM 0.1260 mL 0.6302 mL 1.2604 mL 3.1511 mL
30 mM 0.1050 mL 0.5252 mL 1.0504 mL 2.6259 mL
40 mM 0.0788 mL 0.3939 mL 0.7878 mL 1.9694 mL
50 mM 0.0630 mL 0.3151 mL 0.6302 mL 1.5755 mL
60 mM 0.0525 mL 0.2626 mL 0.5252 mL 1.3130 mL
80 mM 0.0394 mL 0.1969 mL 0.3939 mL 0.9847 mL
100 mM 0.0315 mL 0.1576 mL 0.3151 mL 0.7878 mL
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Tosposertib 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:

Tosposertib1418305-55-1TU2218TU 2218TU-2218Anaplastic lymphoma kinase (ALK)VEGFRAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Vascular endothelial growth factor receptorTGFβVEGFALK5VEGFR2Immuno-oncologyInhibitorinhibitorinhibit

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