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FGFR1/DDR2 inhibitor 1

COA COA
    级别和纯度:
  • ≥98%
有货

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货号 (SKU) 包装规格 是否现货 价格 数量
F651919-1mg
 1mg 现货 Stock Image
F651919-5mg
 5mg 现货 Stock Image
F651919-10mg
 10mg 现货 Stock Image
F651919-25mg
 25mg 现货 Stock Image
大包装询价 收藏夹 比较  SDS下载  DATASHEET  质量标准
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Discoidin Domain Receptor (18) FGFR (112) Protein Tyrosine Kinase/RTK (1319) Receptor Tyrosine Kinase (2808)
main product photo

基本描述

别名 3-(3-(1-环丙基-1H-吡唑-4-基)-1H-吲唑-6-基)-4-甲基-N-(3-(三氟甲基)苯基)苯甲酰胺 | FGFR1/DDR2 抑制剂 1
英文别名 3-(3-(1-Cyclopropyl-1H-pyrazol-4-yl)-1H-indazol-6-yl)-4-methyl-N-(3-(trifluoromethyl)phenyl)benzamide
规格或纯度 ≥98%
英文名称 FGFR1/DDR2 inhibitor 1
生化机理 FGFR1/DDR2 抑制剂 1 是一种具有口服活性的成纤维细胞生长因子受体 1（FGFR1）和 Discoindin 结构域受体 2（DDR2）抑制剂，其 IC 50 值分别为 31.1 nM 和 3.2 nM。抗肿瘤活性。
储存温度 -20°C储存
运输条件 超低温冰袋运输
作用类型 抑制剂
产品介绍


FGFR1/DDR2 inhibitor 1 is an orally active inhibitor of fibroblast growth factor receptor 1 (FGFR1) and discoindin domain receptor 2 (DDR2) , with IC 50 values of 31.1 nM and 3.2 nM, respectively. Antitumor activity

In Vitro

FGFR1/DDR2 inhibitor 1 (compound 11k) (25-200 μM; 2 hours) shows significant inhibition of FGFR2 phosphorylation in a dose-dependent manner in SNU16 cells. FGFR1/DDR2 inhibitor 1 shows (60-250 μM; 2 hours) significant inhibition of DDR2 phosphorylation in a dose-dependent manner in H2286 cells. FGFR1/DDR2 inhibitor 1 significantly inhibits the proliferation of FGFR-driven cancer cell lines with IC 50 s of 108.4, 93.4, 31.8 and 306.6 nM against KG-1, SNU-16, NCI-H716 and UMUC14 respectively. FGFR1/DDR2 inhibitor 1 demonstrates substantially activity against the DDR2-driven cancer cell line NCI-H2286 (93.0 nM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

FGFR1/DDR2 inhibitor 1 (10-20 mg/kg; p.o.; once daily for 7 days) has profound anti-tumor efficacy in NCI-H1581 tumor model . SCID mice bearing NCI-H2286 tumors were randomized and treated with FGFR1/DDR2 inhibitor 1 at doses of 10 mg/kg for 10 consecutive days. FGFR1/DDR2 inhibitor 1 could suppress tumor growth with tumor growth inhibition rates (TGI) of 82.8% . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Nude mice bearing NCI-H1581 tumors Dosage: 10 or 20 mg/kg Administration: P.o.; once daily for 7 days Result: Suppressed tumor growth in a dose-dependent manner with tumor growth inhibition rates (TGI) of 59.7% and 98.1% at doses of 10 and 20 mg/kg, respectively.

Form:Solid

IC50& Target:FGFR1 31.1 nM (IC 50 ) DDR2 3.2 nM (IC 50 )
纯度 ≥98%

关联靶点（人）

DDR2 Tchem 含盘状结构域受体 2(Discoidin domain-containing receptor 2) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
EGFR Tclin Epidermal growth factor receptor erbB1 (33727 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
KCNH2 Tclin HERG (29587 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ERBB2 Tclin Receptor protein-tyrosine kinase erbB-2 (7851 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PDGFRB Tclin Platelet-derived growth factor receptor beta (5195 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
IGF1R Tclin Insulin-like growth factor I receptor (8605 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
FGFR2 Tclin Fibroblast growth factor receptor 2 (3405 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
FGFR1 Tclin Fibroblast growth factor receptor 1 (9149 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SRC Tclin Tyrosine-protein kinase SRC (10310 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CDK6 Tclin Cyclin-dependent kinase 6 (1724 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
JAK1 Tclin Tyrosine-protein kinase JAK1 (8569 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
JAK2 Tclin Tyrosine-protein kinase JAK2 (12915 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
FLT1 Tclin Vascular endothelial growth factor receptor 1 (6262 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
KDR Tclin Vascular endothelial growth factor receptor 2 (20924 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PTK2 Tclin Focal adhesion kinase 1 (4730 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP2D6 Tclin Cytochrome P450 2D6 (33882 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MET Tclin Hepatocyte growth factor receptor (10718 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
EPHB2 Tchem Ephrin type-B receptor 2 (1899 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MAPK3 Tchem MAP kinase ERK1 (4725 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CDK1 Tchem Cyclin-dependent kinase 1 (3927 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP1A2 Tchem Cytochrome P450 1A2 (26471 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PDGFRA Tclin Platelet-derived growth factor receptor alpha (5682 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
FLT3 Tclin Tyrosine-protein kinase receptor FLT3 (13481 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ERBB4 Tclin Receptor protein-tyrosine kinase erbB-4 (2748 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CSF1R Tclin Macrophage colony stimulating factor receptor (5179 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP2C9 Tchem Cytochrome P450 2C9 (32119 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP2C19 Tchem Cytochrome P450 2C19 (29246 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
TEK Tclin Tyrosine-protein kinase TIE-2 (3348 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
EPHA2 Tclin Ephrin type-A receptor 2 (3499 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SNU-16 (476 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
KG-1 (867 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
BTK Tclin Tyrosine-protein kinase BTK (8973 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AXL Tchem Tyrosine-protein kinase receptor UFO (3469 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ALK Tclin ALK tyrosine kinase receptor (7132 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DDR2 Tchem Discoidin domain-containing receptor 2 (2199 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NCI-H1581 (382 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NCI-H716 (90 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

关联靶点（其它种属）

Cdk4 Cyclin-dependent kinase 4 (3 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Mapk1 MAP kinase ERK2 (650 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Fgfr4 Fibroblast growth factor receptor 4 (138 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Fgfr3 Fibroblast growth factor receptor 3 (21 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

名称和识别符

分子类型 未知
IIUPAC Name 3-[3-(1-cyclopropylpyrazol-4-yl)-1H-indazol-6-yl]-4-methyl-N-[3-(trifluoromethyl)phenyl]benzamide
INCHI 1S/C28H22F3N5O/c1-16-5-6-18(27(37)33-21-4-2-3-20(13-21)28(29,30)31)11-24(16)17-7-10-23-25(12-17)34-35-26(23)19-14-32-36(15-19)22-8-9-22/h2-7,10-15,22H,8-9H2,1H3,(H,33,37)(H,34,35)
InChi Key ZEOWTGPWHLSLOG-UHFFFAOYSA-N
Smiles CC1=C(C=C(C=C1)C(=O)NC2=CC=CC(=C2)C(F)(F)F)C3=CC4=C(C=C3)C(=NN4)C5=CN(N=C5)C6CC6
Isomeric SMILES CC1=C(C=C(C=C1)C(=O)NC2=CC=CC(=C2)C(F)(F)F)C3=CC4=C(C=C3)C(=NN4)C5=CN(N=C5)C6CC6
PubChem CID 138454761
分子量 501.5

化学和物理性质

溶解性 DMSO : 250 mg/mL (498.50 mM; Need ultrasonic)
分子量 501.500 g/mol
XLogP3 5.700
氢键供体数Hydrogen Bond Donor Count 2
氢键受体数Hydrogen Bond Acceptor Count 6
可旋转键计数Rotatable Bond Count 5
精确质量Exact Mass 501.178 Da
单同位素质量Monoisotopic Mass 501.178 Da
拓扑极表面积Topological Polar Surface Area 75.600 Ų
重原子数Heavy Atom Count 37
形式电荷Formal Charge 0
复杂度Complexity 822.000
同位素原子数Isotope Atom Count 0
定义的原子立体中心计数Defined Atom Stereocenter Count 0
未定义的原子立体中心计数Undefined Atom Stereocenter Count 0
定义的键立体中心计数Defined Bond Stereocenter Count 0
未定义的键立体中心计数Undefined Bond Stereocenter Count 0
所有立体化学键的总数The total count of all stereochemical bonds 0
共价键合单元计数Covalently-Bonded Unit Count 1

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批号(Lot Number) 证书类型 货号
C2507413 分析证书 F651919
C2507415 分析证书 F651919
C2507416 分析证书 F651919
C2507417 分析证书 F651919
C2507418 分析证书 F651919
C2507419 分析证书 F651919
C2507414 分析证书 F651919
C2507420 分析证书 F651919

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  1. FGFR1/DDR2 inhibitor 1
    FGFR1/DDR2 inhibitor 1
    • 10mM in DMSO

    ¥3,740.90

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