2. Immunology/Inflammation Cell Cycle/DNA Damage
  3. SphK PERK
  4. 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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ABC294735

ABC294735 Chemical Structure

CAS No. : 917236-13-6

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ABC294735 Related Antibodies

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SphK1 SphK2

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Description

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[1].

IC50 & Target[1]

SphK1

 

SphK2

 

In Vitro

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.

ABC294735 Related Antibodies

Western Blot Analysis[1]

Cell Line: A-498; Bxpc-3
Concentration: 25 μM
Incubation Time: 48 h
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.
In Vivo

ABC294735 (50 mg/kg; p.o.; daily Monday to Friday) delays renal cell carcinoma xenograft tumor growth, and co-administration with sorafenib enhances tumor cell apoptosis and reduces pro-survival ERK signaling without overt toxicity[1].
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.

Animal Model: SCID mice[1]
Dosage: 50 mg/kg
Administration: p.o.; daily Monday to Friday
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).
Molecular Weight

425.95

Formula

C25H28ClNO3
CAS No.
SMILES

O=C(NCCC1=CC=C(O)C(O)=C1)C23CC4CC(C2)CC(C5=CC=C(Cl)C=C5)(C4)C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ABC294735 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ABC294735917236-13-6ABC 294735ABC-294735SphKPERKSphingosine kinaseProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinasesphingosine kinase 2sphingosine-1-phosphatesphingosine kinase 1MAPK pathwaykidney carcinomapancreatic adenocarcinomahuman pancreatic adenocarcinoma Bxpc-3 cellshuman kidney carcinoma A-498 cellsapoptosissphingosine phosphorylationInhibitorinhibitorinhibit

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