2. Metabolic Enzyme/Protease Cell Cycle/DNA Damage Immunology/Inflammation
  3. DGK PERK Interleukin Related
  4. BMS-986408

BMS-986408 is an orally active inhibitor of DGKα and DGKζ, with IC50 values of 0.0003 μM and 0.002 μM, respectively. BMS-986408 activates intratumoral T cell responses, enhances the priming and expansion of tumor-reactive T cells in tumor-draining lymph nodes, and functions as an immunostimulant. BMS-986408 can be used in the research of tumors.

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

BMS-986408

BMS-986408 Chemical Structure

CAS No. : 2618418-12-3

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BMS-986408 Related Antibodies

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  • Purity & Documentation

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Description

BMS-986408 is an orally active inhibitor of DGKα and DGKζ, with IC50 values of 0.0003 μM and 0.002 μM, respectively. BMS-986408 activates intratumoral T cell responses, enhances the priming and expansion of tumor-reactive T cells in tumor-draining lymph nodes, and functions as an immunostimulant. BMS-986408 can be used in the research of tumors[1].

In Vitro

BMS-986408 (0.5 μM; 1 h) binds to DGKα and DGKζ in Jurkat cells and alters their thermal stability[1].
BMS-986408 (1-100 nM; 1 h) potently induces the translocation of DGKα-YFP (EC50 = 0.026 μmol/L) and DGKζ-YFP (EC50 = 0.008 μmol/L) from the cytoplasm to the plasma membrane in Jurkat cells[1].
BMS-986408 (0.001-10 μM; 24 h) induces dose-dependent degradation of DGKα and DGKζ in human peripheral blood mononuclear cells[1].
BMS-986408 (0.1-1000 nM; 0-24 h) potently enhances T cell activation in human whole blood, induces phosphorylation of ERK in CD4+ T cells (EC50 = 0.008 μM) and CD8+ T cells (EC50 = 0.012 μM), and simultaneously triggers the production of IL2 (EC50 = 0.019-0.034 μM)[1].
BMS-986408 (250 nM; 3 days) enhances the production of cytokines including IFNγ in patient-derived tumorospheres from non-small cell lung cancer (NSCLC) patients[1].

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

BMS-986408 Related Antibodies

Western Blot Analysis[1]

Cell Line: PBMCs
Concentration: 0.001, 0.002, 0.005, 0.013, 0.04, 0.12, 0.37, 1.1, 3.3, 10 μM
Incubation Time: 24 h
Result: Reduced the levels of DGKα and DGKζ in a dose dependent-manner.
In Vivo

BMS-986408 (0.3 mg/kg; p.o.; once daily; 28 days) significantly enhances the complete tumor response rate when combined with anti-PD-1 therapy in C57BL/6 or Balb/c mice inoculated with MC38, CT26 or SA1N tumor cells[1].

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

Animal Model: C57BL/6 mice (female, 8-10 weeks old) and Balb/c mice (female, 8-10 weeks old); C57BL/6 mice were subcutaneously injected with MC38 tumor cells, Balb/c mice were subcutaneously injected with CT26 or SA1N tumor cells[1]
Dosage: 0.3 mg/kg
Administration: p.o.; once daily; 28 days
Result: Exhibited tumor growth inhibition but no complete responses (CRs) in all three tumor models.
Achieved robust therapeutic responses with 90% to 100% CRs with anti-PD-1.
Clinical Trial
Molecular Weight

512.57

Formula

C27H31F3N6O
CAS No.
Appearance

Solid

Color

Off-white to light brown

SMILES

CC[C@H]1CN([C@@H](CN1C2=NC(N(C3=CC=C(N=C32)C#N)C)=O)CC)[C@H](C4=CC=C(C=C4)C(F)(F)F)CC
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 (195.10 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 1.9510 mL 9.7548 mL 19.5095 mL
5 mM 0.3902 mL 1.9510 mL 3.9019 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)

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

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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 (4.88 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.88 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:

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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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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 1.9510 mL 9.7548 mL 19.5095 mL 48.7738 mL
5 mM 0.3902 mL 1.9510 mL 3.9019 mL 9.7548 mL
10 mM 0.1951 mL 0.9755 mL 1.9510 mL 4.8774 mL
15 mM 0.1301 mL 0.6503 mL 1.3006 mL 3.2516 mL
20 mM 0.0975 mL 0.4877 mL 0.9755 mL 2.4387 mL
25 mM 0.0780 mL 0.3902 mL 0.7804 mL 1.9510 mL
30 mM 0.0650 mL 0.3252 mL 0.6503 mL 1.6258 mL
40 mM 0.0488 mL 0.2439 mL 0.4877 mL 1.2193 mL
50 mM 0.0390 mL 0.1951 mL 0.3902 mL 0.9755 mL
60 mM 0.0325 mL 0.1626 mL 0.3252 mL 0.8129 mL
80 mM 0.0244 mL 0.1219 mL 0.2439 mL 0.6097 mL
100 mM 0.0195 mL 0.0975 mL 0.1951 mL 0.4877 mL
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BMS-986408 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:

BMS-9864082618418-12-3BMS986408BMS 986408DGKPERKInterleukin RelatedDiacylglycerol kinaseProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseILT cellsJurkat T cellsDGKαHEK293A cellsPD-1 therapyDGKζnon-small cell lung cancerCAR T-cell therapyInhibitorinhibitorinhibit

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