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Soquelitinib

SKU: orb2565260

Description

Soquelitinib (CPI-818) is an oral, covalent inhibitor of ITK that selectively reduces Th2 cytokine production. It demonstrates anti-tumor activity in mouse models by modulating T-cell function, reducing exhaustion markers, and enhancing tumor infiltration alongside the upregulation of CXCR3, IFNγ, and CD107a in CD8+ T cells. This profile supports its research use in immunology and oncology for studying T-cell-mediated responses.

Research Area

Cell Biology, Immunology & Inflammation, Neuroscience, Pharmacology & Drug Discovery, Signal Transduction

Images & Validation

Key Properties

CAS Number2226636-04-8
MW514.66
Purity99.54%
FormulaC25H30N4O4S2
SMILESC(=O)(C1=C(OC)C=C(C)C(SC=2SC(NC(=O)C3CC3)=NC2)=C1)N4C[C@@H](C)N(C(C=C)=O)CCC4
TargetTyrosine Kinases,CXCR,COX,TNF,IL Receptor,Immunology/Inflammation related
SolubilityDMSO:80 mg/mL (155.44 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:10 mg/mL (19.43 mM)

Bioactivity

Target IC50
IL-2 secretion (Jurkat T cells):136 nM
In Vivo
Oral administration of soquelitinib (30 mg/kg, b.i.d.) significantly inhibited tumor growth in multiple murine tumor models (CT26, RENCA, B16F10, EL4, A20). Soquelitinib enhanced CD8+ T-cell infiltration and cytotoxic activity (e.g., increased IFNγ, TNF, Perforin). Combined treatment with anti-PD-1 or CTLA-4 antibodies showed synergistic effects, with complete tumor regression in some cases and reduced expression of exhaustion markers in TILs. Long-term oral dosing in rats showed no observable toxicity (NOAEL >1000 mg/kg).
In Vitro
In Jurkat T cells, Soquelitinib inhibits downstream TCR signaling (e.g., phosphorylation of PLCγ1 and ERK) and suppresses IL-2 secretion (IC₅₀ = 136 nM). Soquelitinib downregulates Th2 cytokines (IL-4, IL-5, IL-13) and promotes Th1 skewing. In repeatedly stimulated human CD8 T cells, 1 μM soquelitinib reduces exhaustion markers (PD1, LAG3, TIGIT, Tim3) and restores effector functions, increasing IFNγ and Granzyme B levels.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

CPI818, CPI-818
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Key Properties

No computed properties available.

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Protocol Information

Soquelitinib (orb2565260)

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% DMSO +
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% Tween 80 +
%

Available Sizes

Select a size below

1 mg
¥ 2,860.00
5 mg
¥ 6,240.00
1 ml x 10 mM (in DMSO)
¥ 6,890.00
10 mg
¥ 9,880.00
25 mg
¥ 18,980.00
50 mg
¥ 28,210.00
100 mg
¥ 38,090.00
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