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.
For research use only. We do not sell to patients.
- CAS No.: 3065226-39-0
- Formula: C29H20N6O
- Molecular Weight:468.51
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Darlifarnib
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Biological Activity
Description
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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CAS No. 3065226-39-0
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Appearance Solid
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Molecular Weight 468.51
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Formula C29H20N6O
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Color White to off-white
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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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
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
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (106.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.34 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.34 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (286 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.1344 mL | 10.6721 mL | 21.3443 mL | 53.3607 mL |
| 5 mM | 0.4269 mL | 2.1344 mL | 4.2689 mL | 10.6721 mL | |
| 10 mM | 0.2134 mL | 1.0672 mL | 2.1344 mL | 5.3361 mL | |
| 15 mM | 0.1423 mL | 0.7115 mL | 1.4230 mL | 3.5574 mL | |
| 20 mM | 0.1067 mL | 0.5336 mL | 1.0672 mL | 2.6680 mL | |
| 25 mM | 0.0854 mL | 0.4269 mL | 0.8538 mL | 2.1344 mL | |
| 30 mM | 0.0711 mL | 0.3557 mL | 0.7115 mL | 1.7787 mL | |
| 40 mM | 0.0534 mL | 0.2668 mL | 0.5336 mL | 1.3340 mL | |
| 50 mM | 0.0427 mL | 0.2134 mL | 0.4269 mL | 1.0672 mL | |
| 60 mM | 0.0356 mL | 0.1779 mL | 0.3557 mL | 0.8893 mL | |
| 80 mM | 0.0267 mL | 0.1334 mL | 0.2668 mL | 0.6670 mL | |
| 100 mM | 0.0213 mL | 0.1067 mL | 0.2134 mL | 0.5336 mL |
Darlifarnib Related Classifications
HY-172423 Related Classifications
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Keywords
- Darlifarnib
- 3065226-39-0
- KO-2806
- KO2806
- KO 2806
- Farnesyl Transferase
- mTOR
- VEGFR
- Ftase
- Mammalian target of Rapamycin
- Vascular endothelial growth factor receptor
- tyrosine kinase inhibitors
- RHEB
- primary human umbilical vein endothelial cells
- anti-VEGFR TKIs
- Caki1 renal cell carcinoma xenografts
- apoptosis
- mTORC1
- endothelial cells
- cell cycle arrest
- renal cell carcinoma
- Inhibitor
- inhibitor
- inhibit