| Identification | Back Directory | [Name]
Cyclopropanecarboxamide, N-[5-[[5-[[(3R)-hexahydro-3-methyl-4-(1-oxo-2-propen-1-yl)-1H-1,4-diazepin-1-yl]carbonyl]-4-methoxy-2-methylphenyl]thio]-2-thiazolyl]- | [CAS]
2226636-04-8 | [Synonyms]
soquelitinib
Soquelitinib (CPI-818)
Cyclopropanecarboxamide, N-[5-[[5-[[(3R)-hexahydro-3-methyl-4-(1-oxo-2-propen-1-yl)-1H-1,4-diazepin-1-yl]carbonyl]-4-methoxy-2-methylphenyl]thio]-2-thiazolyl]- | [Molecular Formula]
C25H30N4O4S2 | [MOL File]
2226636-04-8.mol | [Molecular Weight]
514.66 |
| Chemical Properties | Back Directory | [density ]
1.34±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
8.15±0.70(Predicted) | [color ]
White to off-white | [InChIKey]
KNCWSXRTKLTULH-MRXNPFEDSA-N | [SMILES]
C1(C(NC2=NC=C(SC3=CC(C(N4CCCN(C(=O)C=C)[C@H](C)C4)=O)=C(OC)C=C3C)S2)=O)CC1 |
| Hazard Information | Back Directory | [Uses]
Soquelitinib (CPI-818) is an orally active and highly selective covalent interleukin-2-inducible kinase (ITK) inhibitor. Soquelitinib is active in six different models of T cell-mediated inflammatory and immune disease, including acute and chronic asthma, pulmonary fibrosis, systemic sclerosis (scleroderma), psoriasis, and acute graft versus host disease with Th2 cytokine product inhibition. Soquelitinib increases tumor infiltration of normal CD8+ cells that possess enhanced T effector function[1][2][3]. | [in vivo]
Soquelitinib (30 mg/kg, oral gavage, twice daily for 20 days) enhances CD8T cell infiltration, increases cytolytic capacity of tumor-infiltrating lymphocytes (TILs) and enhances anti-PD1 and anti-CTLA4 efficacy in the CT26 tumor model[1].
| Animal Model: | Murine syngeneictumor models[2] | | Dosage: | 30 mg/kg | | Administration: | oral gavage, twice daily for 20 days | | Result: | Induced significantly higher frequency of intra-tumoral CD8 T cells in the CT26 model and a moderate increase in intra-tumoral CD8 infiltration.
Augmented the antitumor efficacy of immune checkpoint blockade, leading to durable antitumor response in the CT26 model. |
| [References]
[1] Hsu L Y, et al. Selective inhibition of interleukin-2 inducible T cell kinase (ITK) enhances anti-tumor immunity in association with Th1-skewing, cytotoxic T cell activation, and reduced T cell exhaustion[J]. bioRxiv, 2023: 2023.07. 05.547822.
[2] Ding N, et al. Dynamic Single-Cell Profiling Reveals Novel Immune Regulatory Mechanism of ITK Inhibitor Soquelitinib in Refractory T Cell Lymphoma [J]. Blood, 2023, 142: 1442.
[3] Hsu L Y, et al. Soquelitinb, A selective inhibitor of interleukin-2-inducible kinase (ITK), is active in several murine models of T cell-mediated inflammatory disease[J]. bioRxiv, 2023: 2023.10. 27.564296. |
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| Company Name: |
CAREBIO PHARMA Gold
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| Tel: |
18501057619 18501057619; |
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