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.
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- CAS No.: 917236-13-6
- Formule: C25H28ClNO3
- Masse moléculaire:425.95
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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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).
Chemical Information
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CAS No. 917236-13-6
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Masse moléculaire 425.95
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ABC294735 Related Classifications
HY-112385 Related Classifications
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- 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