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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 3065226-39-0
- 分子式: C29H20N6O
- 分子量:468.51
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Darlifarnib
MoreVEGFR アイソフォーム固有の製品をすべて表示
More
生物活性
|
mTORC1 |
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 (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.
化学情報
-
CAS 番号 3065226-39-0
-
分子量 468.51
-
分子式 C29H20N6O
-
SMILES
N#CC1=CC(C2=CC(OCC3=CC([C@@]4(C5=CN=CN5C)N)=CC=C3C#N)=CC=C2)=C6C=C4C=CC6=N1
-
別名
KO-2806
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
-
Journal Impact Factor
-
Most Recent
-
Cancer Res
The Farnesyl Transferase Inhibitor Darlifarnib (KO-2806) Resensitizes Relapsing Tumors to RAS Inhibition. [Abstract]2026 Feb 9. PMID: 41661652
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Darlifarnib 関連分類
HY-172423 関連分類
Powered by Bioz