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托瑞尼布

强效的PDGFR和VEGFR抑制剂

规格或纯度: ≥98%

CAS编号: 356068-94-5
分子式: C₂₂H₂₅FN₄O₂
分子量: 396.46
PubChem编号: 5329106

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货号 (SKU)	包装规格	是否现货
T126745-10mg	10mg	现货
T126745-50mg	50mg	现货
T126745-250mg	250mg	现货

查看相关系列

fibroblast growth factor receptor 1 Inhibitor kinase insert domain receptor Inhibitor platelet derived growth factor receptor alpha Inhibitor

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基本描述

规格或纯度	≥98%
英文名称	Toceranib
别名	SU 11654;PHA 291639
英文别名	SU 11654;PHA 291639;SU11654;SU-11654;PHA-291639;PHA291639; 5-[(Z)-(5-Fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-N-[2-(1-pyrrolidinyl)ethyl]-1H-pyrrole-3-carboxamide
生化机理	有力的ATP竞争性PDGFR和VEGFR抑制剂（Ki分别为5和6 nM）；抑制c-Kit的磷酸化并抑制表达突变Kit的肥大细胞系的生长，诱导细胞周期停滞和凋亡。还抑制FGFR1（Ki =0.5μM）。在体内有效。
储存温度	-20°C储存
运输条件	超低温冰袋运输
备注	50mg、10mg卖完停产，不再备货
产品介绍	Toceranib(SU 11654; PHA 291639)是激酶抑制剂，有抗肿瘤和抗血管生成活性，能抑制KIT，VEGFR2和PDGFRβ。 Toceranib(SU 11654; PHA 291639) is a kinase inhibitor with both antitumor and antiangiogenic activity through inhibition of KIT, vascular endothelial growth factor receptor 2, and PDGFRβ.

名称和标识符

IUPAC Name	5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-N-(2-pyrrolidin-1-ylethyl)-1H-pyrrole-3-carboxamide
INCHI	InChI=1S/C22H25FN4O2/c1-13-19(12-17-16-11-15(23)5-6-18(16)26-21(17)28)25-14(2)20(13)22(29)24-7-10-27-8-3-4-9-27/h5-6,11-12,25H,3-4,7-10H2,1-2H3,(H,24,29)(H,26,28)/b17-12-
InChi Key	SRSGVKWWVXWSJT-ATVHPVEESA-N
Canonical SMILES	CC1=C(NC(=C1C(=O)NCCN2CCCC2)C)C=C3C4=C(C=CC(=C4)F)NC3=O
分子式	C₂₂H₂₅FN₄O₂
PubChem CID	5329106
分子量	396.46

数据库链接

PubChem CID	5329106
CAS Registry No.	356068-94-5
ChEMBL Ligand	CHEMBL13608
BindingDB Ligand	4818
RCSB PDB Ligand	BWC

化学和物理性质

溶解性	溶于DMSO, 最高浓度 (mg/mL): 3.96, 最高浓度(mM): 10 温和加热

靶标

Target ID

1803

名称

platelet derived growth factor receptor alpha

缩写名

PDGFRα

家族

Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family

别名

mrgG

基因和蛋白信息

Species	Transmembrane Domains	Amino Acids	Chromosomal Location	Gene Symbol	Gene Name
Human	1	1089	4q12	PDGFRA	platelet derived growth factor receptor alpha
Mouse	1	1089	5 39.55 cM	Pdgfra	platelet derived growth factor receptor, alpha polypeptide
Rat	1	1088	14p11	Pdgfra	platelet derived growth factor receptor alpha

Ensembl Gene

ENSG00000134853 (Hs) , ENSMUSG00000029231 (Mm) , ENSRNOG00000002244 (Rn)

Entrez Gene

18595 (Mm) , 25267 (Rn) , 5156 (Hs)

OMIM

173490 (Hs)

Protein GI

158186636 (Rn) , 134032050 (Mm) , 5453870 (Hs)

UniProtKB

P16234 (Hs) , P20786 (Rn) , P26618 (Mm)

RefSeq Nucleotide

NM_001083316 (Mm) , NM_006206 (Hs) , NM_012802 (Rn)

RefSeq Protein

NP_001076785 (Mm) , NP_006197 (Hs) , NP_035188 (Mm) , NP_036934 (Rn)

Orphanet

124154 (Hs)

DrugBank Target

P16234 (Hs)

CATH/Gene3D

2.60.40.10 (N/A)

ChEMBL Target

CHEMBL2007 (Hs) , CHEMBL3466 (Mm)

Target ID

1808

名称

fibroblast growth factor receptor 1

缩写名

FGFR1

家族

Type V RTKs: FGF (fibroblast growth factor) receptor family

别名

MRGG

基因和蛋白信息

Species	Transmembrane Domains	Amino Acids	Chromosomal Location	Gene Symbol	Gene Name
Human	1	822	8p11.23	FGFR1	fibroblast growth factor receptor 1
Mouse	1	822	8 14.12 cM	Fgfr1	fibroblast growth factor receptor 1
Rat	1	822	16q12.4	Fgfr1	Fibroblast growth factor receptor 1

Ensembl Gene

ENSG00000077782 (Hs) , ENSMUSG00000031565 (Mm) , ENSRNOG00000016050 (Rn)

Entrez Gene

14182 (Mm) , 79114 (Rn) , 2260 (Hs)

OMIM

136350 (Hs)

Protein GI

13162333 (Rn) , 291327497 (Hs) , 120952698 (Mm)

UniProtKB

P11362 (Hs) , P16092 (Mm) , Q04589 (Rn)

RefSeq Nucleotide

NM_001174063 (Hs) , NM_010206 (Mm) , NM_024146 (Rn)

RefSeq Protein

NP_001073377 (Mm) , NP_001073378 (Mm) , NP_034336 (Mm) , NP_056934 (Hs) , NP_077060 (Rn)

Orphanet

121802 (Hs)

DrugBank Target

P11362 (Hs)

CATH/Gene3D

2.60.40.10 (N/A)

ChEMBL Target

CHEMBL3650 (Hs) , CHEMBL4523276 (Rn) , CHEMBL3960 (Mm)

Target ID

1813

名称

kinase insert domain receptor

缩写名

VEGFR-2

家族

Type IV RTKs: VEGF (vascular endothelial growth factor) receptor family

别名

EBRT2

基因和蛋白信息

Species	Transmembrane Domains	Amino Acids	Chromosomal Location	Gene Symbol	Gene Name
Human	1	1356	4q12	KDR	kinase insert domain receptor
Mouse	1	1367	5 40.23 cM	Kdr	kinase insert domain protein receptor
Rat	1	1343	14p11	Kdr	kinase insert domain receptor

Ensembl Gene

ENSG00000128052 (Hs) , ENSMUSG00000062960 (Mm) , ENSRNOG00000046829 (Rn)

Entrez Gene

16542 (Mm) , 25589 (Rn) , 3791 (Hs)

OMIM

191306 (Hs)

Protein GI

11321597 (Hs) , 27777648 (Mm) , 6981128 (Rn)

UniProtKB

P35968 (Hs) , P35918 (Mm) , O08775 (Rn)

RefSeq Nucleotide

NM_002253 (Hs) , NM_010612 (Mm) , NM_013062 (Rn)

RefSeq Protein

NP_002244 (Hs) , NP_034742 (Mm) , NP_037194 (Rn)

Orphanet

229801 (Hs)

DrugBank Target

P35968 (Hs)

CATH/Gene3D

2.60.40.10 (N/A)

ChEMBL Target

CHEMBL3337 (Mm) , CHEMBL279 (Hs)

关联配体

Ligand ID	11619
名称	toceranib
别名	PHA-291639
类别	Synthetic organic
学名	4-amino-N-(4,6-dimethylpyrimidin-2-yl)benzenesulfonamide
生物活性评价	The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in ).
评价	Toceranib (PHA-291639 and formerly SU11654) is a small molecule, multi-targeted receptor tyrosine kinase inhibitor . It is structurally related to . Targets include VEGFRs, FGFR, PDGFRs, and Kit (including constitutively active mutant forms ). Like sunitinib, toceranib has antiangiogenic and anitproliferative actions. Palladiar® branded toceranib is used to treat solid tumours in dogs.

参考文献

1. Liao AT, Chien MB, Shenoy N, Mendel DB, McMahon G, Cherrington JM, London CA. (2002) Inhibition of constitutively active forms of mutant kit by multitargeted indolinone tyrosine kinase inhibitors.. Blood, 100 (2): (585-93). [PMID:12091352]
2. Sun L, Liang C, Shirazian S, Zhou Y, Miller T, Cui J, Fukuda JY, Chu JY, Nematalla A, Wang X et al.. (2003) Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase.. J Med Chem, 46 (7): (1116-9). [PMID:12646019]