2. Protein Tyrosine Kinase/RTK Immunology/Inflammation
  3. c-Fms TAM Receptor MHC
  4. Adrixetinib TFA

Adrixetinib TFA  (Synonyms: Q702 TFA)

Cat. No.: HY-152830A Purity: 99.82%
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Handling Instructions Technical Support

Adrixetinib (Q702) TFA is an orally active triple inhibitor against CSF1R, Mer, and Axl, with Kd values of 8.7 nM, 0.8 nM, and 0.3 nM, respectively. Adrixetinib TFA acts as a potent immune modulator that remodels the tumor microenvironment. Adrixetinib TFA increases the abundance of M1 macrophages and CD8⁺ T cells, while decreasing the levels of M2 macrophages and myeloid-derived suppressor cells (MDSCs). Adrixetinib TFA upregulates the expression of MHC class I and E-cadherin in tumor cells. Adrixetinib TFA shows remarkable antitumor efficacy in syngeneic mouse tumor models. Adrixetinib TFA is suitable for the research of breast cancer, renal adenocarcinoma, colon carcinoma, and melanoma.

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

Adrixetinib TFA

Adrixetinib TFA Chemical Structure

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Adrixetinib TFA:

Adrixetinib TFA Related Antibodies

Top Publications Citing Use of Products

View All TAM Receptor Isoform Specific Products:

View All Isoforms
Axl Mer Tyro3

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View All Isoforms
MHC I MHC II

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Adrixetinib (Q702) TFA is an orally active triple inhibitor against CSF1R, Mer, and Axl, with Kd values of 8.7 nM, 0.8 nM, and 0.3 nM, respectively. Adrixetinib TFA acts as a potent immune modulator that remodels the tumor microenvironment. Adrixetinib TFA increases the abundance of M1 macrophages and CD8⁺ T cells, while decreasing the levels of M2 macrophages and myeloid-derived suppressor cells (MDSCs). Adrixetinib TFA upregulates the expression of MHC class I and E-cadherin in tumor cells. Adrixetinib TFA shows remarkable antitumor efficacy in syngeneic mouse tumor models. Adrixetinib TFA is suitable for the research of breast cancer, renal adenocarcinoma, colon carcinoma, and melanoma[1][2].

IC50 & Target

Axl

0.3 nM (Kd)

Mer

0.8 nM (Kd)

MHC I

 

In Vitro

Adrixetinib (Q702; 1 h) TFA potently binds to and inhibits purified Axl, Mer, and CSF1R kinases with IC50 values of 0.3 nM, 0.8 nM, and 8.7 nM, respectively[1].
Adrixetinib (0.001-10 μM; 24 h pretreatment) TFA concentration-dependently inhibits Gas6-induced phosphorylation of Axl and AKT in H1299 cells, concentration-dependently inhibits Gas6-induced phosphorylation of Mer and AKT in A549 cells, and concentration-dependently inhibits CSF1-induced phosphorylation of CSF1R and ERK in THP-1 cells[1].
Adrixetinib (0.1-100 μM; 72 h) TFA directly inhibits EMT6 cell viability with an IC50 of 8.4 μM[1].
Adrixetinib TFA inhibits M-NFS-60 cell proliferation through the CSF1R pathway with an IC50 < 1.0 μM, showing potent cellular activity[2].

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

Adrixetinib TFA Related Antibodies
In Vivo

Adrixetinib (Q702; 30 mg/kg; p.o.; daily; 7 days) TFA inhibits Axl and CSF1R phosphorylation in subcutaneous xenograft tumors in nude mice[1].
Adrixetinib (10-100 mg/kg; p.o.; daily; 14 days) TFA induces dose-dependent tumor growth control (54.3% to 84.6%) in subcutaneous EMT6 syngeneic breast cancer tumors in BALB/c mice[1].
Adrixetinib (30 mg/kg; p.o.; daily; up to 7 days) TFA modulates EMT6 gene expression in subcutaneous EMT6 tumors to promote an immune-stimulatory microenvironment in BALB/c mice[1].
Adrixetinib (30 mg/kg; p.o.; daily; 5 to 22 days) TFA remodels the immune cell population in subcutaneous MHC-I and E-cadherin expression in BALB/c mice[1].
Adrixetinib (30 mg/kg; p.o.; daily; 7 days) TFA enhances the effector function of T and natural killer cells by increasing IFN-γ and granzyme B production in both subcutaneous EMT6 tumors and peripheral blood of BALB/c mice[1].
Adrixetinib (30 mg/kg; p.o.; daily; 21 days) TFA increases CD8 T cell infiltration, reduces myeloid cell accumulation, and upregulates MHC-I and PD-L1 expression in subcutaneous EMT6 tumors in BALB/c mice[1].
Adrixetinib (30 mg/kg; p.o.; daily; 9 days) TFA increases tumor antigen-specific CD8 T cell infiltration into subcutaneous B16F10-OVA melanoma tumors in C57BL/6 mice[1].
Adrixetinib (30 mg/kg; p.o.; daily; up to 27 days) TFA induces tumor growth inhibition (64% to 77% TGI) in subcutaneous CT26, MC38, and RENCA syngeneic tumor models in mice[1].

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

645.51

Formula

C27H25F6N5O7
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=NN(CCC)C=C1OCC(F)(F)F)NC2=NC=C(C=C2)OC3=C4C=C(OC)C(OC)=CC4=NC=C3.OC(C(F)(F)F)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (154.92 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 1.5492 mL 7.7458 mL 15.4916 mL
5 mM 0.3098 mL 1.5492 mL 3.0983 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 (sealed storage, away from moisture). 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
=
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 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.
Calculation results:
Working solution concentration: mg/mL
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 (sealed storage, away from moisture). 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 1.5492 mL 7.7458 mL 15.4916 mL 38.7291 mL
5 mM 0.3098 mL 1.5492 mL 3.0983 mL 7.7458 mL
10 mM 0.1549 mL 0.7746 mL 1.5492 mL 3.8729 mL
15 mM 0.1033 mL 0.5164 mL 1.0328 mL 2.5819 mL
20 mM 0.0775 mL 0.3873 mL 0.7746 mL 1.9365 mL
25 mM 0.0620 mL 0.3098 mL 0.6197 mL 1.5492 mL
30 mM 0.0516 mL 0.2582 mL 0.5164 mL 1.2910 mL
40 mM 0.0387 mL 0.1936 mL 0.3873 mL 0.9682 mL
50 mM 0.0310 mL 0.1549 mL 0.3098 mL 0.7746 mL
60 mM 0.0258 mL 0.1291 mL 0.2582 mL 0.6455 mL
80 mM 0.0194 mL 0.0968 mL 0.1936 mL 0.4841 mL
100 mM 0.0155 mL 0.0775 mL 0.1549 mL 0.3873 mL
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Adrixetinib TFA 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:

AdrixetinibQ702Q 702Q-702c-FmsTAM ReceptorMHCCSF-1 receptorcolony stimulating factor 1 receptorCSF-1RCSF1RTyro3AxlMerMajor Histocompatibility Complexproteintyrosine kinaseantineoplasticcancerInhibitorinhibitorinhibit

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