TNG917
TNG917 is a potent, selective EHMT1/2 inhibitor with oral activity. TNG917 reduces H3K9me2-mediated transcriptional repression, restores interferon-stimulated gene expression, promotes the secretion of T-cell chemokines such as CXCL10, and converts immunologically cold tumors into T-cell inflamed tumors. TNG917 is applicable to studies on immunologically cold tumors, colorectal cancer, anti-tumor immunity, interferon signaling pathways and epigenetic immune escape.
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- CAS No.: 2923223-81-6
- 화학식: C20H24FN5O
- 분자량:369.44
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
All Histone Methyltransferase Isoforms
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Biological Activity
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EHMT1 |
EHMT2 |
TNG917 dose-dependently reduces H3K9me2 levels in cells, with a cellular potency IC50 of approximately 2 nM, and induces CXCL10 secretion with an AC50 of approximately 5 nM[1].
TNG917 (1-10 μM) is a selective inhibitor of EHMT1/2, and exerts no significant inhibitory effect on the other 37 tested methyltransferases at concentrations of 1 μM and 10 μM[1].
TNG917 relieves H3K9-mediated transcriptional repression, restores the expression of interferon-stimulated genes, and induces the secretion of T cell chemokines such as CXCL10[2].
TNG917 (1 μM) upregulates interferon-stimulated genes in human colorectal cancer cell line HT29, mimicking the phenotype of EHMT1/2 double knockout[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
TNG917 (10-100 mg/kg, p.o.; once daily for 5 consecutive days) exhibits dose-dependent plasma exposure in female C57BL/6 mice bearing MC38 tumors, and reduces H3K9me2 levels in tumor tissues at 2 and 8 h after the final administration[1].
Combination treatment with TNG917 (3, 30 mg/kg, p.o.; once daily for 6 consecutive days) and Pembrolizumab (HY-P9902A) (10 mg/kg, i.p.; once weekly for a total of 3 times) increases the infiltration of total T cells, CD8+ T cells, CD4+ T cells and M1 macrophages, and reduces M2 macrophages within CT26 tumors[1].
Combination treatment with TNG917 (30 mg/kg, p.o.) and Pembrolizumab (10 mg/kg, i.p.) induces chemokines such as Ccl8, Ccl5 and Ccl3, as well as interferon-stimulated gene-related signals in CT26 tumor tissues[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (female, MC38 tumor-bearing)[1]
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Dosage:10 mg/kg; 30 mg/kg; 100 mg/kg
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Administration:p.o.; daily; 5 days
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Result:Produced dose-dependent plasma exposure and reduced tumor H3K9me2 levels at 2 and 8 h after the final dose.
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Animal Model:NOG (HT29 human colon carcinoma tumor-bearing，immunodeficient)[1]
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Dosage:3 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:p.o.; once daily
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Result:Inhibited tumor growth, with tumor growth inhibition of 50% and 84% at 10 and 30 mg/kg, respectively.
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Animal Model:BALB/c (female，CT26 syngeneic tumor-bearing)[1]
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Dosage:TNG917: 3 mg/kg; 30 mg/kg; Pembrolizumab: 10 mg/kg
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Administration:TNG917: p.o.; once daily for 6 days;Pembrolizumab: i.p.; once weekly for 3 doses; tumors collected on Day 7
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Result:Increased intratumoral T cells, CD8+ T cells, CD4+ T cells and M1 macrophages, and decreased M2 macrophages.
Chemical Information
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CAS No. 2923223-81-6
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분자량 369.44
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화학식 C20H24FN5O
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SMILES
FC(C(C1=CCNCCC1)=C2OCCC2=C3)=C3NC4=NC(C)=CC(NC)=N4
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TNG917 Related Classifications
HY-184500 Related Classifications
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