ABC294735
ABC294735 is an orally active SK1/SK2 inhibitor. Combination of ABC294735 with Sorafenib (HY-10201) reduces pERK. ABC294735 exhibits anticancer activity against pancreatic adenocarcinoma and renal cell carcinoma. ABC294735 can be used in research related to pancreatic adenocarcinoma and renal cell carcinoma.
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。
- CAS 番号: 917236-13-6
- 分子式: C25H28ClNO3
- 分子量:425.95
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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
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SphK1 |
SphK2 |
ABC294735 (48 h) inhibits proliferation of human kidney carcinoma A-498 cells with an IC50 of 20 μM and human pancreatic adenocarcinoma Bxpc-3 cells with an IC50 of 40 μM after 48 hours of exposure[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A-498; Bxpc-3
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Concentration:25 μM
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Incubation Time:48 h
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Result:Synergized with Sorafenib to reduce the levels of phosphorylated ERK1/2 (pERK).
Synergized with Gemcitabin to reduce the levels of phosphorylated ERK1/2 (pERK).
Did not show changes in total ERK1/2 protein.
ABC294735 (50 mg/kg; p.o.; daily Monday to Friday) delays pancreatic adenocarcinoma xenograft tumor growth without overt toxicity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID mice[1]
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Dosage:50 mg/kg
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Administration:p.o.; daily Monday to Friday
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Result:Delayed tumor growth in the xenograft model.
Increased tumor growth inhibition when co-administered with sorafenib, though this decrease did not reach statistical significance.
Increased numbers of TUNEL-positive apoptotic cells in tumors when co-administered with sorafenib compared to single-agent treatment.
Reduced p-ERK levels in A-498 tumors when co-administered with sorafenib.
Caused no significant mouse weight loss or increased apoptotic cells in normal tissues (small intestine, liver).
化学情報
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CAS 番号 917236-13-6
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分子量 425.95
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分子式 C25H28ClNO3
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SMILES
O=C(NCCC1=CC=C(O)C(O)=C1)C23CC4CC(C2)CC(C5=CC=C(Cl)C=C5)(C4)C3
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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)
- ABC294735
- 917236-13-6
- ABC 294735
- ABC-294735
- SphK
- PERK
- sphingosine kinase 2
- sphingosine-1-phosphate
- sphingosine kinase 1
- MAPK pathway
- kidney carcinoma
- pancreatic adenocarcinoma
- human pancreatic adenocarcinoma Bxpc-3 cells
- human kidney carcinoma A-498 cells
- apoptosis
- sphingosine phosphorylation
- Inhibitor
- inhibitor
- inhibit