Home Other Building Blocks TSU-68 (Random Configuration)

TSU-68 (Random Configuration)

CAS No.:
252916-29-3
Catalog Number:
AG0037HX
Molecular Formula:
C18H18N2O3
Molecular Weight:
310.3471
Pack Size
Purity
Availability
Location
Price(USD)
Quantity
  
1mg
≥98%
1 week
United States
$90
- +
5mg
≥98%
1 week
United States
$139
- +
10mg
≥98%
1 week
United States
$194
- +
50mg
98%
1 week
United States
$657
- +
100mg
98%
1 week
United States
$1107
- +
Product Description
Catalog Number:
AG0037HX
Chemical Name:
TSU-68 (Random Configuration)
CAS Number:
252916-29-3
Molecular Formula:
C18H18N2O3
Molecular Weight:
310.3471
MDL Number:
MFCD09743433
IUPAC Name:
3-[2,4-dimethyl-5-[(Z)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid
InChI:
InChI=1S/C18H18N2O3/c1-10-12(7-8-17(21)22)11(2)19-16(10)9-14-13-5-3-4-6-15(13)20-18(14)23/h3-6,9,19H,7-8H2,1-2H3,(H,20,23)(H,21,22)/b14-9-
InChI Key:
NHFDRBXTEDBWCZ-ZROIWOOFSA-N
SMILES:
OC(=O)CCc1c(C)[nH]c(c1C)C=C1C(=O)Nc2c1cccc2
UNII:
9RL37ZZ665
NSC Number:
702827
Properties
Complexity:
516  
Compound Is Canonicalized:
Yes
Covalently-Bonded Unit Count:
1  
Defined Atom Stereocenter Count:
0
Defined Bond Stereocenter Count:
1  
Exact Mass:
310.132g/mol
Formal Charge:
0
Heavy Atom Count:
23  
Hydrogen Bond Acceptor Count:
3  
Hydrogen Bond Donor Count:
3  
Isotope Atom Count:
0
Molecular Weight:
310.353g/mol
Monoisotopic Mass:
310.132g/mol
Rotatable Bond Count:
4  
Topological Polar Surface Area:
82.2A^2
Undefined Atom Stereocenter Count:
0
Undefined Bond Stereocenter Count:
0
XLogP3:
2.2  
Literature
Title Journal
A phase I pharmacokinetic study of TSU-68 (a multiple tyrosine kinase inhibitor of VEGFR-2, FGF and PDFG) in combination with S-1 and oxaliplatin in metastatic colorectal cancer patients previously treated with chemotherapy. Investigational new drugs 20120801
The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. Bioorganic & medicinal chemistry letters 20120801
Novel tricyclic indeno[2,1-d]pyrimidines with dual antiangiogenic and cytotoxic activities as potent antitumor agents. Bioorganic & medicinal chemistry 20120715
N⁴-(3-Bromophenyl)-7-(substituted benzyl) pyrrolo[2,3-d]pyrimidines as potent multiple receptor tyrosine kinase inhibitors: design, synthesis, and in vivo evaluation. Bioorganic & medicinal chemistry 20120401
Augmentation of chemotherapeutic infusion effect by TSU-68, an oral targeted antiangiogenic agent, in a rabbit VX2 liver tumor model. Cardiovascular and interventional radiology 20120201
Phase I clinical study of the angiogenesis inhibitor TSU-68 combined with carboplatin and paclitaxel in chemotherapy-naive patients with advanced non-small cell lung cancer. Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20120201
Evaluation of molecular targeted cancer drug by changes in tumor marker doubling times. Journal of gastroenterology 20120101
Acenaphtho[1,2-b]pyrrole-based selective fibroblast growth factor receptors 1 (FGFR1) inhibitors: design, synthesis, and biological activity. Journal of medicinal chemistry 20110609
Phase I, pharmacokinetic, and biological studies of TSU-68, a novel multiple receptor tyrosine kinase inhibitor, administered after meals with solid tumors. Cancer chemotherapy and pharmacology 20110501
Phase I and pharmacokinetic study of TSU-68, a novel multiple receptor tyrosine kinase inhibitor, by twice daily oral administration between meals in patients with advanced solid tumors. Cancer chemotherapy and pharmacology 20110501
A phase I/II trial of the oral antiangiogenic agent TSU-68 in patients with advanced hepatocellular carcinoma. Cancer chemotherapy and pharmacology 20110201
Synthesis and biological activity of N(4)-phenylsubstituted-6-(2,4-dichloro phenylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic and antitumor agents. Bioorganic & medicinal chemistry 20100515
5-Substituted pyrido[2,3-d]pyrimidine, an inhibitor against three receptor tyrosine kinases. Bioorganic & medicinal chemistry letters 20090201
TSU68, an antiangiogenic receptor tyrosine kinase inhibitor, induces tumor vascular normalization in a human cancer xenograft nude mouse model. Surgery today 20090101
TSU68 prevents liver metastasis of colon cancer xenografts by modulating the premetastatic niche. Cancer research 20081201
Identification of human liver cytochrome P450 isoforms involved in autoinduced metabolism of the antiangiogenic agent (Z)-5-[(1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-propanoic acid (TSU-68). Drug metabolism and disposition: the biological fate of chemicals 20080601
Time-dependent induction of rat hepatic CYP1A1 and CYP1A2 expression after single-dose administration of the anti-angiogenic agent TSU-68. Drug metabolism and pharmacokinetics 20080101
The selectivity of protein kinase inhibitors: a further update. The Biochemical journal 20071215
Decrease in plasma concentrations of antiangiogenic agent TSU-68 ((Z)-5-[(1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-propanoic acid) during oral administration twice a day to rats. Drug metabolism and disposition: the biological fate of chemicals 20070901
Novel inhibitor for fibroblast growth factor receptor tyrosine kinase. Bioorganic & medicinal chemistry letters 20070901
Potent platelet-derived growth factor-beta receptor (PDGF-betaR) inhibitors: Synthesis and structure-activity relationships of 7-[3-(cyclohexylmethyl)ureido]-3-{1-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl}quinoxalin-2(1H)-one derivatives. Chemical & pharmaceutical bulletin 20070201
Dose-finding study of the multitargeted tyrosine kinase inhibitor SU6668 in patients with advanced malignancies. Clinical cancer research : an official journal of the American Association for Cancer Research 20050901
Inhibition of peritoneal dissemination of ovarian cancer by tyrosine kinase receptor inhibitor SU6668 (TSU-68). International journal of cancer 20050320
Vascular endothelial growth factor: a therapeutic target for tumors of the Ewing's sarcoma family. Clinical cancer research : an official journal of the American Association for Cancer Research 20050315
Combined inhibition of vascular endothelial growth factor and platelet-derived growth factor signaling: effects on the angiogenesis, microcirculation, and growth of orthotopic malignant gliomas. Journal of neurosurgery 20050201
Combined antiangiogenic and immune therapy of prostate cancer. Angiogenesis 20050101
In vivo assessment of antiangiogenic activity of SU6668 in an experimental colon carcinoma model. Clinical cancer research : an official journal of the American Association for Cancer Research 20040115
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. Journal of medicinal chemistry 20030327
Design, synthesis, and evaluations of substituted 3-[(3- or 4-carboxyethylpyrrol-2-yl)methylidenyl]indolin-2-ones as inhibitors of VEGF, FGF, and PDGF receptor tyrosine kinases. Journal of medicinal chemistry 19991216
Properties