FPTI
FPTI is a SYT-SSX1 fusion protein modulator with selective cytotoxicity in SYT-SSX1-positive synovial sarcoma cells. FPTI down-regulates SYT-SSX1 expression and modulates its downstream target genes. FPTI induces apoptosis in synovial sarcoma cells. FPTI can be used for the research of synovial sarcoma.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 173374-58-8
- 分子式: C15H10FN5
- 分子量:279.27
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
体外実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Yamato (SYT-SSX1-positive synovial sarcoma), ASKA (SYT-SSX1-positive synovial sarcoma), HEK293 (immortalized embryonic kidney), 143B (sarcoma), A673 (sarcoma)
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Concentration:10-100 μM (72 h); 40 μM (24, 48, 96 h)
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Incubation Time:24 h, 48 h, 72 h, 96 h
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Result:Reduced cell viability by 48.71% in HEK293, 67.35% in ASKA, and 72.48% in Yamato cells at 40 μM for 72 h compared to DMSO controls.
Showed insignificant cytotoxicity at 10 μM and 20 μM.
Induced cytotoxicity in HEK293 cells below 50% viability at 60, 80, 100 μM.
Showed no significant cytotoxicity in 143B or A673 cells.
Achieved IC50 values of 39 μM for ASKA, 33 μM for Yamato, 66 μM for HEK293, 64 μM for 143B, and 70 μM for A673.
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Cell Line:ASKA (SYT-SSX1-positive synovial sarcoma)
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Concentration:10 μM, 40 μM (72 h)
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Incubation Time:72 h
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Result:Downregulated expression of SYT-SSX1 and its downstream target genes cyclin D1 (CCDN1), β-catenin (CTNNB1), FZD, PDGFRA, COM1, SMARCB1, and P21 at 40 μM.
Induced dose-dependent repression of FZD, CCDN1, SMARCB1, and P21.
Downregulated EGFR and EGR1 only at 10 μM.
Upregulated CDKN2A with treatment.
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Cell Line:ASKA (SYT-SSX1-positive synovial sarcoma)
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Concentration:10 μM (IC10), 40 μM (IC50) (24 h)
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Incubation Time:24 h
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Result:Altered cell forward and side scatter parameters compared to untreated cells.
Increased cell death to over twice the basal level at 10 μM.
Increased cell death to thrice the basal level at 40 μM.
Induced a marked increase in dual Annexin V/PI staining indicative of late apoptosis at 40 μM.
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Cell Line:ASKA (SYT-SSX1-positive synovial sarcoma)
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Concentration:10 μM (non-lethal dose), 40 μM (IC50) (72 h)
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Incubation Time:72 h
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Result:Increased the sub-G0 cell population to 31.25% (from 5.385% in untreated cells) and reduced the G0-G1 population to 44.9% (from 69.1% in untreated cells) at 40 μM.
Left the S and G2/M phase populations nearly unchanged at 40 μM.
Increased the sub-G0 population to 15.3% and reduced the G0-G1 population to 53.5% at 10 μM.
- RNA extraction experimental
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Cell Cytotoxicity Assay
- Mammalian live/dead viability and cytotoxicity staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- Apoptosis Solutions
- Cell Viability Determination by MTT Colorimetric Assay
化学情報
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CAS 番号 173374-58-8
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分子量 279.27
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分子式 C15H10FN5
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SMILES
FC1=CC=C2NC=C(C2=C1)C3=NN=NN3C4=CC=CC=C4
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)