2. Metabolic Enzyme/Protease Immunology/Inflammation Stem Cell/Wnt MAPK/ERK Pathway
  3. DGK IFNAR Interleukin Related ERK
  4. Alcudacigib

Alcudacigib (ASP1570; DGKζ-IN-1) 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 selectively inhibits the kinase activity of DGKζ and induces proteasome-dependent degradation of DGKζ protein. Alcudacigib enhances the anti-tumor functions of T cells and NK cells. Alcudacigib can be used for the research of advanced/metastatic solid tumors.

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Alcudacigib

Alcudacigib Chemical Structure

CAS No. : 2660218-70-0

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Alcudacigib Related Antibodies

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Description

Alcudacigib (ASP1570; DGKζ-IN-1) 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 selectively inhibits the kinase activity of DGKζ and induces proteasome-dependent degradation of DGKζ protein. Alcudacigib enhances the anti-tumor functions of T cells and NK cells. Alcudacigib can be used for the research of advanced/metastatic solid tumors[1][2].

IC50 & Target[2]

ERK1

 

ERK2

 

IL-2

 

In Vitro

Alcudacigib (0.1 μM; 5-30 min) 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) 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) degrades the DGKζ protein in Jurkat and B16F1 cells through a proteasome-dependent mechanism[2].
Alcudacigib (0.0003-1 μM; 30 min) 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) enhances IL-2 production in TCR-stimulated Jurkat cells[2].
Alcudacigib (0.0001-1 μM; 3 days) 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) 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) 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) 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.

Alcudacigib Related Antibodies

Western Blot Analysis[2]

Cell Line: Jurkat (human T-cell line), B16F1 (mouse melanoma cell line)
Concentration: 0.1, 1, 10, 100 and 1000 nM (Jurkat cells); 1 μM (B16F1 cells)
Incubation Time: 24 h (Jurkat cells); 5 h (B16F1 cells, with 30 min pre-incubation with MG-132 or DMSO)
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.
In Vivo

Alcudacigib (0.1-10 mg/kg; p.o.; once daily or twice daily for 10 consecutive days) dose-dependently inhibits the growth of MC38 colon adenocarcinoma in mice[2].
Alcudacigib (0.1-3 mg/kg; p.o.; once daily or twice daily for 9-10 consecutive days) 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) 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) 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.

Animal Model: C57BL/6J (5-week-old female, subcutaneously inoculated with 2×105 MC38 colon adenocarcinoma cells)[2]
Dosage: 0.1 mg/kg; 0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg; 5 mg/kg (twice daily)
Administration: p.o.; once daily; 10 days; twice daily; 10 days
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.
Animal Model: C57BL/6J (5- to 6-week-old female, subcutaneously inoculated with 1×105 B16F1 melanoma cells)[2]
Dosage: 5 mg/kg (twice daily); 0.1 mg/kg; 0.3 mg/kg; 1 mg/kg; 3 mg/kg
Administration: p.o.; twice daily; 10 days; once daily; 9 days
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.
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]
Dosage: 3 mg/kg
Administration: p.o.; once daily; 10 days
Result: Induced marked tumor growth inhibition, but this effect was completely abolished by CD8+ T-cell depletion.
Animal Model: C57BL/6J (female, healthy)[2]
Dosage: 3 mg/kg
Administration: p.o.; single dose
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.
Molecular Weight

554.59

Formula

C27H25F3N6O2S
CAS No.
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
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Alcudacigib Related Classifications

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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:

Alcudacigib2660218-70-0DGKζ-IN-1DGKIFNARInterleukin RelatedERKDiacylglycerol kinaseInterferon-α/β receptorInterferon-alpha/beta receptor ILExtracellular signal regulated kinasescancerNK cellB16F1 cellsJurkat cellsIFNγcolon adenocarcinomamelanomaC57BL/6J miceDiacylglycerol kinase ζ (DGKζ)T-cellInhibitorinhibitorinhibit

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