製品番号: HY-108713

Famitinib

(別名: SHR1020)

カスタマーレビュー

Based on 1 Customer Validation

Famitinib (SHR1020), an orally active multi-targeted kinase inhibitor, inhibits the activity of c-kit, VEGFR-2 and PDGFRβ with IC₅₀ values of 2.3 nM, 4.7 nM and 6.6 nM, respectively. Famitinib exerts powerful antitumor activity in human gastric cancer cells and xenografts. Famitinib triggers apoptosis.

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純度: 98.13%
CAS 番号: 1044040-56-3
分子式: C₂₃H₂₇FN₄O₂
分子量:410.48

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Famitinib 構造式

CAS 番号: 1044040-56-3

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
- 臨床実験
化学情報
溶剤 & 溶解度
- 体外
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

Famitinib (SHR1020), an orally active multi-targeted kinase inhibitor, inhibits the activity of c-kit, VEGFR-2 and PDGFRβ with IC₅₀ values of 2.3 nM, 4.7 nM and 6.6 nM, respectively^[1]. Famitinib exerts powerful antitumor activity in human gastric cancer cells and xenografts. Famitinib triggers apoptosis^[2].

IC₅₀ & Target^[2]

VEGFR-2

4.2 nM (IC₅₀)

PDGFRβ

6.6 nM (IC₅₀)

c-kit

2.3 nM (IC₅₀)

VEGFR アイソフォーム固有の製品をすべて表示 :

PDGFR アイソフォーム固有の製品をすべて表示 :

体外実験

Famitinib inhibits the VEGF-induced proliferation, migration and tubule formation of human umbilical vein endothelial cells, and micro-vessel spouting from matrigel-embedded rat aortic rings^[1].
Famitinib (1.8 and 3.6 μM; 48 h) inhibits cell proliferation by inducing cell cycle arrest at the G2/M phase and causes cell apoptosis in a dose-dependent manner in gastric cancer cell lines^[2].
Famitinib (0.6-20.0 μM; 24-72 h) inhibits gastric cancer cell growth in a dose-dependent manner^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[2]

Cell Line:

Human gastric cancer cells BGC-823 and MGC-803
Concentration:

0, 0.6, 1.25, 2.5, 5.0, 10.0 and 20.0 µM
Incubation Time:

24, 48 and 72 hours
Result:

Inhibited cell growth in a dose-dependent manner with IC₅₀ values of 3.6 and 3.1 µM for BGC-823 and MGC-803 cells, respectively.

体内実験

Famitinib exhibits broad and potent anti-tumor activity, leading to regression or growth arrest of various established xenografts derived from human tumor cell lines ^[1].
Famitinib (50 and 100 mg/kg; p.o. once daily for 3 weeks) reduces tumor growth in vivo via inhibition of angiogenesis^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

18-20 g female BALB/c athymic nu/nu mice (age, 6–8 weeks) bearing BGC-823 xenografts^[2]
Dosage:

50 and 100 mg/kg
Administration:

Oral gavage; 50 and 100 mg/kg; once daily for 3 weeks
Result:

Inhibited BGC-823 xenograft growth (tumor volume, 395.2 vs. 2,690.5 mm³), and animal weights were similar between groups (21.6 vs. 18.7 g).

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 1044040-56-3
性状 Solid
分子量 410.48
分子式 C₂₃H₂₇FN₄O₂
Color Yellow to orange
SMILES

O=C1C2=C(NC(/C=C3C(NC4=C\3C=C(F)C=C4)=O)=C2C)CCN1CCN(CC)CC
別名

SHR1020
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

DMSO : 2.86 mg/mL (6.97 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4362 mL

12.1809 mL

24.3617 mL

5 mM

0.4872 mL

2.4362 mL

4.8723 mL

10 mM

---

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.

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (274 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Liguang Lou, et al. Abstract 3604: Preclinical antitumor study of famitinib, an orally available multi-targeted kinase inhibitor of VEGFR/PDGFR/c-Kit in phase I clinical trials.

[2]. Sai Ge, et al. Famitinib exerted powerful antitumor activity in human gastric cancer cells and xenografts. Oncol Lett. 2016 Sep;12(3):1763-1768. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
DMSO	1 mM	2.4362 mL	12.1809 mL	24.3617 mL	60.9043 mL
DMSO	5 mM	0.4872 mL	2.4362 mL	4.8723 mL	12.1809 mL

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Famitinib

Apoptosis Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Covalent Screening Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Human Metabolite Library

Anti-Pulmonary Fibrosis Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cytokine Inhibitors Library

Cell Death Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

VEGFR アイソフォーム固有の製品をすべて表示

PDGFR アイソフォーム固有の製品をすべて表示