2. Metabolic Enzyme/Protease PI3K/Akt/mTOR Protein Tyrosine Kinase/RTK
  3. Farnesyl Transferase mTOR VEGFR
  4. Darlifarnib

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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Darlifarnib

Darlifarnib Chemical Structure

CAS No. : 3065226-39-0

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Darlifarnib Related Antibodies

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1 Publications Citing Use of MCE Darlifarnib

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Description

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[1].

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.

Darlifarnib Related Antibodies
In Vivo

Darlifarnib (10 mg/kg; p.o.; twice daily; for 42 consecutive days) as a single agent induces tumor stasis, and in combination with anti-VEGFR TKIs, achieves durable tumor regression in Caki1 renal cell carcinoma xenografts[1].
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.

Animal Model: BALB/c nude mice[1]
Dosage: 10 mg/kg
Administration: p.o.; twice daily; 42 days
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.
Animal Model: BALB/c nude mice; NOD/SCID mice (for KI-12-0097 PDX)[1]
Dosage: 20 mg/kg (KI-12-0073 PDX)
Administration: p.o.; twice daily; 28-31 days
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.
Molecular Weight

468.51

Formula

C29H20N6O
CAS No.
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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Purity & Documentation
References
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Darlifarnib Related Classifications

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  • 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:

Darlifarnib3065226-39-0KO-2806KO2806KO 2806Farnesyl TransferasemTORVEGFRFtaseMammalian target of RapamycinVascular endothelial growth factor receptortyrosine kinase inhibitorsRHEBprimary human umbilical vein endothelial cellsanti-VEGFR TKIsCaki1 renal cell carcinoma xenograftsapoptosismTORC1endothelial cellscell cycle arrestrenal cell carcinomaInhibitorinhibitorinhibit

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