Darlifarnib
Based on 1 publication(s) in Google Scholar
Darlifarnib (KO-2806) is an orally active farnesyl transferase inhibitor. Darlifarnib inhibits the mTORC1 signaling pathway, thereby enhancing the anti-angiogenic properties of tyrosine kinase inhibitors. When used in combination with anti-VEGFR tyrosine kinase inhibitors, Darlifarnib promotes renal cell carcinoma tumor regression and inhibits tumor neovascularization. Darlifarnib sensitizes renal cell carcinoma tumors that progress after anti-VEGFR TKI treatment.
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- No. CAS: 3065226-39-0
- Fòrmula: C29H20N6O
- Peso molecular:468.51
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Publications Citing Use of MedChemExpress (MCE) Darlifarnib
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
mTORC1 |
In Vitro
Darlifarnib (5-500 nM; 7 days) enhances the antiproliferative activity of anti-VEGFR TKIs in primary umbilical vein endothelial cells[1].
Combination treatment with darlifarnib (250 nM; 96 h) and an anti-VEGFR TKI (Axitinib (HY-10065), Lenvatinib (HY-10981), or Cabozantinib (HY-13016)) induces significantly higher levels of apoptosis in HUVEC cells compared to treatment with either agent alone[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Darlifarnib (20 mg/kg for KI-12-0073; p.o.; twice daily; 28-31 days) enhances cabozantinib-mediated tumor growth inhibition, induces tumor cell cycle arrest in multiple renal cell carcinoma xenograft models, and the combination treatment significantly reduces tumor angiogenesis and achieves durable tumor regression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice[1]
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Dosage:10 mg/kg
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Administration:p.o.; twice daily; 42 days
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Result:Induced tumor stasis, with mean percent tumor volume change near 0% at day 42.
Drove durable tumor regressions when combined with axitinib, lenvatinib, or cabozantinib, with mean percent tumor volume changes reaching negative values (tumor shrinkage) at day 42.
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Animal Model:BALB/c nude mice; NOD/SCID mice (for KI-12-0097 PDX)[1]
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Dosage:20 mg/kg (KI-12-0073 PDX)
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Administration:p.o.; twice daily; 28-31 days
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Result:Enhanced tumor growth inhibition across all tested models when combined with Cabozantinib, inducing tumor regressions in 4 out of 6 models.
Led to more rapid and durable tumor regression than cabozantinib in the KI-12-0073 PDX model.
Significantly reduced CD31-positive endothelial area and NG2-positive pericyte area compared to cabozantinib in KI-12-0073 tumors after 14 days of treatment.
Chemical Information
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No. CAS 3065226-39-0
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Peso molecular 468.51
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Fòrmula C29H20N6O
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SMILES
N#CC1=CC(C2=CC(OCC3=CC([C@@]4(C5=CN=CN5C)N)=CC=C3C#N)=CC=C2)=C6C=C4C=CC6=N1
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Synonyms
KO-2806
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Cancer Res
The Farnesyl Transferase Inhibitor Darlifarnib (KO-2806) Resensitizes Relapsing Tumors to RAS Inhibition. [Abstract]2026 Feb 9. PMID: 41661652
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Darlifarnib Related Classifications
HY-172423 Related Classifications
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