NCP26 TFA
Based on 1 Customer Validation
NCP26 TFA is an ATP-competitive ProRS inhibitor (with a KD of 271 nM in the absence of proline, and a KD of 0.35 nM in the presence of 100 μM proline). NCP26 TFA activates AAR, induces G0/G1 phase arrest, Apoptosis, Caspase cleavage, and PARP cleavage. NCP26 TFA downregulates MYC, TCF3, and CCND1. NCP26 TFA inhibits the growth of multiple myeloma cells. NCP26 TFA can be used for the research of multiple myeloma.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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。
- 分子式: C22H24F3N5O4
- 分子量:479.45
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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生物活性
製品説明
IC50 & Target
[1]|
Caspase 8 |
Caspase 9 |
Caspase 3 |
体外実験
NCP26 TFA is an ATP-competitive inhibitor of recombinant ProRS. Its binding affinity increases by more than 750-fold in the presence of 100 μM proline, with a KD of 0.35 nM[1].
NCP26 (0.5 μM; 48 h) TFA maintains antiproliferative activity against AMO1 and RPMI 8226 multiple myeloma (MM) cells over a proline concentration range of 0 to 20 mM, with no reduction in its potency at high proline levels[1].
NCP26 (0.01-10 μM; 96 h) TFA is 10-fold more potent against AMO1 multiple myeloma (MM) cells than against peripheral blood mononuclear cells (PBMCs) from healthy donors, with an EC50 of 0.1 μM for the former and approximately 1 μM for the latter after 96 h of treatment[1].
NCP26 TFA potently inhibits the growth of most multiple myeloma (MM) cell lines, with EC50 values ranging from 135 nM to 1.1 μM[1].
NCP26 (0.5 μM; 6-48 h) TFA induces G0/G1 cell cycle arrest and caspase-dependent apoptosis in AMO1 and RPMI 8226 multiple myeloma (MM) cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:AMO1, RPMI 8226 MM cell lines
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Concentration:0.5 μM
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Incubation Time:6 h, 24 h, 48 h
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Result:Induced G0/G1 cell cycle arrest in both cell lines at 6 h, with enhanced arrest observed at 24 h.
Induced apoptotic cell death, evidenced by increased Annexin-V+ cells, sub-G1 populations, and mitochondrial damage.
Induced time- and dose-dependent cleavage of caspases-3, -8, -9, and PARP.
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Cell Line:AMO1, RPMI 8226 MM cell lines
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Concentration:0-1 μM
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Incubation Time:6 h
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Result:Dose-dependently reduced protein levels of MYC, PIM2, CCND1, and TCF3 in both cell lines.
Mirrored the effects of EPRS shRNA knockdown on MYC, PIM2, CCND1, and TCF3 protein levels.
体内実験
NCP26 (10 mg/kg; q.d. [daily]) TFA significantly inhibits multiple myeloma tumor growth (P = 0.005) and prolongs host survival (P < 0.001) in an AMO1 xenograft mouse model without inducing weight loss[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CB17 SCID (5-week-old female, subcutaneously inoculated with AMO1 cells)[1]
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Dosage:2.5 mg/kg; 10 mg/kg
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Administration:i.p.; once daily; 21 days
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Result:Significantly inhibited AMO1 tumour growth compared to vehicle control (control vs.
2.5 mg/kg, P = 0.01; control vs.
10 mg/kg, P < 0.001).
Resulted in greater tumour growth inhibition at 10 mg/kg dose than 2.5 mg/kg dose.
Caused no significant body weight loss in either treatment cohort.
Significantly prolonged overall survival compared to vehicle control (control vs.
2.5 mg/kg, P = 0.01; control vs.
10 mg/kg, P < 0.001).
Downregulated MYC, CCND1, and TCF3, and induced p-GCN2 and DDIT3 in treated tumours.
化学情報
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性状 Solid
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分子量 479.45
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分子式 C22H24F3N5O4
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SMILES
O=C(C1=NC=CN=C1NC(N2CCCCC2)=O)NC3CC4=C(C3)C=CC=C4.O=C(O)C(F)(F)F
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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)
NCP26 TFA 関連分類
HY-183004A 関連分類
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