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

Adrixetinib TFA  (Synonyms: Q702 TFA)

製品番号: HY-152830A 純度: 99.82%
COA 取扱説明書 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.

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Adrixetinib TFA

Adrixetinib TFA 構造式

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 964 在庫あり
Solution
10 mM * 1 mL in DMSO USD 964 在庫あり
Solid
5 mg $679 在庫あり
10 mg $1087 在庫あり
25 mg $2175 在庫あり
50 mg $3480 在庫あり
100 mg   お問い合わせ  
200 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 0 publication(s) in Google Scholar

Other Forms of Adrixetinib TFA:

Adrixetinib TFA 関連抗体

Top Publications Citing Use of Products

TAM Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Axl Mer Tyro3

MHC アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
MHC I MHC II

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  • 純度とドキュメンテーション

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製品説明

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

 

体外実験

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 関連抗体
体内実験

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.
分子量

645.51

分子式

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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture

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

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
10 mM 0.1549 mL 0.7746 mL 1.5492 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
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Concentration
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Volume
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Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

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体積 （終了）

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
純度とドキュメンテーション
参考文献

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

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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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製品名:
Adrixetinib TFA
製品番号:
HY-152830A
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