Alcudacigib TFA
Based on 1 Customer Validation
Alcudacigib (ASP1570; DGKζ-IN-1) TFA is an orally active diacylglycerol kinase ζ (DGKζ) inhibitor, with an IC50 of 4.7 nM against human DGKζ and an IC50 of 3.0 nM against mouse DGKζ. Alcudacigib TFA selectively inhibits the kinase activity of DGKζ and induces proteasome-dependent degradation of DGKζ protein. Alcudacigib TFA enhances the anti-tumor functions of T cells and NK cells. Alcudacigib TFA can be used for the research of advanced/metastatic solid tumors.
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- Pureté: 99.13%
- Formule: C29H26F6N6O4S
- Masse moléculaire:668.61
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Alcudacigib (0.1 μM; 5-30 min) TFA enhances DAG-mediated ERK phosphorylation in DX5+ NK cells isolated from the spleens of wild-type mice stimulated with anti-NK1.1[1].
Alcudacigib (0.001-1 μM; 5 h) TFA dose-dependently enhances IFN-γ production and degranulation in CD4/8-DX5+NKp46+ NK cells from wild-type mouse spleens stimulated with anti-NK1.1[1].
Alcudacigib (0.1-1000 nM; 5.5-24.5 h) TFA degrades the DGKζ protein in Jurkat and B16F1 cells through a proteasome-dependent mechanism[2].
Alcudacigib (0.0003-1 μM; 30 min) TFA enhances the downstream signaling pathway of DAG in TCR-stimulated Jurkat cells, which is evidenced by statistically significant increases in the phosphorylation levels of PKD and ERK1/2[2].
Alcudacigib (0.0003-1 μM; 24 h) TFA enhances IL-2 production in TCR-stimulated Jurkat cells[2].
Alcudacigib (0.0001-1 μM; 3 days) TFA enhances the proliferation, IL-2 production and IFN-γ production of human primary CD8+ T cells activated via TCR[2].
Alcudacigib (0.0001-1 μM; 3 days) TFA restores and enhances the activation of primary human CD8+ T cells (including cell viability, IL-2 production, and IFN-γ production) that is inhibited by TGF-β1, PGE2 or AMP[2].
Alcudacigib (0.0001-1 μM; 3 days) TFA enhances proliferation, IL-2 production and IFN-γ production of primary mouse CD8+ T cells stimulated by TCR[2].
Alcudacigib (0.0003-3 μM; 24 h) TFA completely reverses PD-1-mediated T cell suppression and partially reverses CTLA-4- and TIGIT-mediated T cell suppression in cellular assays[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Jurkat (human T-cell line), B16F1 (mouse melanoma cell line)
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Concentration:0.1, 1, 10, 100 and 1000 nM (Jurkat cells); 1 μM (B16F1 cells)
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Incubation Time:24 h (Jurkat cells); 5 h (B16F1 cells, with 30 min pre-incubation with MG-132 or DMSO)
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Result:Induced dose-dependent degradation of DGKζ protein in Jurkat cells.
Induced degradation of DGKζ protein in B16F1 cells, which was suppressed by pre-treatment with MG-132, a proteasome inhibitor.
Alcudacigib (0.1-3 mg/kg; p.o.; once daily or twice daily for 9-10 consecutive days) TFA inhibits the growth of CPI-resistant B16F1 melanoma in female C57BL/6J mice[2].
Alcudacigib (3 mg/kg; p.o.; once daily for 10 consecutive days) TFA exerted its antitumor effect against B16F10 melanoma in female C57BL/6J mice in a CD8+T cell-dependent manner[2].
Alcudacigib (3 mg/kg; p.o.; single administration) TFA enhances the expression of T cell activation markers (CD25 and CD69) in splenic CD4+ and CD8+ T cells of healthy female C57BL/6J mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (5-week-old female, subcutaneously inoculated with 2×105 MC38 colon adenocarcinoma cells)[2]
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Dosage:0.1 mg/kg; 0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg; 5 mg/kg (twice daily)
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Administration:p.o.; once daily; 10 days; twice daily; 10 days
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Result:Significantly inhibited tumor growth at doses of 0.3 mg/kg and higher with no effect on mouse body weight.
Showed comparable or superior antitumor efficacy to anti-PD-1 antibody treatment at 5 mg/kg twice daily.
Increased the percentage of intratumoral CD45+, CD3+, CD4+, CD8+, and Treg cells, along with the absolute number of these cell populations, and significantly increased the CD8+/Treg ratio at 3 mg/kg once daily.
Significantly increased the frequency of Ki-67+, CD107a+, CD137+, and PD-1+ cells in both intratumoral CD4+ and CD8+ T cells.
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Animal Model:C57BL/6J (5- to 6-week-old female, subcutaneously inoculated with 1×105 B16F1 melanoma cells)[2]
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Dosage:5 mg/kg (twice daily); 0.1 mg/kg; 0.3 mg/kg; 1 mg/kg; 3 mg/kg
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Administration:p.o.; twice daily; 10 days; once daily; 9 days
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Result:Significantly inhibited B16F1 tumor growth at 5 mg/kg twice daily while anti-PD-1 antibody showed no efficacy.
Significantly inhibited tumor growth at doses of 0.3 mg/kg and higher given once daily with no effect on mouse body weight.
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Animal Model:C57BL/6J (5- to 6-week-old female, subcutaneously inoculated with 5×105 B16F10 melanoma cells, with concurrent anti-CD8 antibody depletions on days 0, 1, 2, 6, and 10)[2]
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Dosage:3 mg/kg
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Administration:p.o.; once daily; 10 days
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Result:Induced marked tumor growth inhibition, but this effect was completely abolished by CD8+ T-cell depletion.
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Animal Model:C57BL/6J (female, healthy)[2]
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Dosage:3 mg/kg
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Administration:p.o.; single dose
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Result:Significantly increased the geometric mean fluorescence intensity of CD25 and CD69 in both splenic CD4+ and CD8+ T cells.
Increased the proportion of CD25+ and CD69+ T cells.
Chemical Information
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Appearance Solid
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Masse moléculaire 668.61
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Formule C29H26F6N6O4S
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Color White to off-white
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SMILES
FC(F)(C1=C(N2C[C@@H](CCC2)CN)C(NC(C3=CSC(C4=CN=NC=C4)=N3)=O)=CC=C1OC5=CC=CC=C5)F.OC(C(F)(F)F)=O
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Synonyms
DGKζ-IN-1 TFA
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
DMSO : 100 mg/mL (149.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.74 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.74 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (281 KB)
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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)
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Instruction de manipulation (2659 KB)
Références
[1]. Okumura M, et al. The diacylglycerol kinase ζ inhibitor ASP1570 augments natural killer cell function. Int Immunopharmacol. 2023;125(Pt A):111145. [Content Brief]
[2]. Ikeda O, et al. Enhanced Antitumor Immunity by ASP1570, a Novel Diacylglycerol Kinase ζ Inhibitor, Offers a Potential Novel Immunotherapy for Treating Cancer. Mol Cancer Ther. 2025;24(6):884-895. [Content Brief]
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 | 1.4956 mL | 7.4782 mL | 14.9564 mL | 37.3910 mL |
| 5 mM | 0.2991 mL | 1.4956 mL | 2.9913 mL | 7.4782 mL | |
| 10 mM | 0.1496 mL | 0.7478 mL | 1.4956 mL | 3.7391 mL | |
| 15 mM | 0.0997 mL | 0.4985 mL | 0.9971 mL | 2.4927 mL | |
| 20 mM | 0.0748 mL | 0.3739 mL | 0.7478 mL | 1.8696 mL | |
| 25 mM | 0.0598 mL | 0.2991 mL | 0.5983 mL | 1.4956 mL | |
| 30 mM | 0.0499 mL | 0.2493 mL | 0.4985 mL | 1.2464 mL | |
| 40 mM | 0.0374 mL | 0.1870 mL | 0.3739 mL | 0.9348 mL | |
| 50 mM | 0.0299 mL | 0.1496 mL | 0.2991 mL | 0.7478 mL | |
| 60 mM | 0.0249 mL | 0.1246 mL | 0.2493 mL | 0.6232 mL | |
| 80 mM | 0.0187 mL | 0.0935 mL | 0.1870 mL | 0.4674 mL | |
| 100 mM | 0.0150 mL | 0.0748 mL | 0.1496 mL | 0.3739 mL |
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