Pelitinib

Suppliers

Names

[ Name ]:
Pelitinib

[Synonym ]:
2-Butenamide,N-[4-[(3-chloro-4-fluorophenyl)amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-,(2E)
4-dimethylamino-but-2-enoic acid [4-(3-chloro-4-fluoro-phenylamino)-3-cyano-7-ethoxy-quinolin-6-yl]-amide
3-Cyano-4-[(3-chlor-4-fluorphenyl)amino]-6-{[4-(N,N-dimethylamino)-1-oxo-2-buten-1-yl]amino}-7-ethoxy-chinoline
(2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide
(2E)-N-{4-[(3-Chloro-4-fluorophenyl)amino]-3-cyano-7-ethoxyquinolin-6-yl}-4-(dimethylamino)but-2-enamide
pelitinib
(2E)-N-[4-[(3-chloro-4-fluorophenyl)amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-buteneamide
WAY-EKB 569
EKB-569
(E)-N-(4-(3-chloro-4-fluorophenylamino)-3-cyano-7-ethoxyquinolin-6-yl)-4-(dimethylamino)but-2-enamide
(2E)-N-{4-[(3-Chloro-4-fluorophenyl)amino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide
2-Butenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-, (2E)-
3-cyano-4-[(3-chloro-4-fluorophenyl)amino]-6-{[4-(N,N-dimethylamino)-1-oxo-2-buten-1-yl]amino}-7-ethoxy-quinoline

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
655.5±55.0 °C at 760 mmHg

[ Melting Point ]:
173-178ºC

[ Molecular Formula ]:
C₂₄H₂₃ClFN₅O₂

[ Molecular Weight ]:
467.923

[ Flash Point ]:
350.2±31.5 °C

[ Exact Mass ]:
467.152435

[ PSA ]:
90.28000

[ LogP ]:
5.95

[ Vapour Pressure ]:
0.0±2.0 mmHg at 25°C

[ Index of Refraction ]:
1.645

[ Storage condition ]:
-20°C Freezer

[ Water Solubility ]:
DMSO: soluble5mg/mL, clear (warmed)

Safety Information

[ Symbol ]:

GHS06

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H301

[ Precautionary Statements ]:
P301 + P310

[ Hazard Codes ]:
T

[ Risk Phrases ]:
25

[ Safety Phrases ]:
45

[ RIDADR ]:
UN 2811 6.1 / PGIII

[ Packaging Group ]:
III

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

Dimethylamine
6-amino-4-(3-chloro-4-fluorophenylamino)-7-ethoxyquinoline-3-carbonitrile
3-Chloro-4-fluoroaniline
5-methoxy-2-methyl-4-nitroaniline
3-ethoxy-4-nitroaniline
2-ACETAMIDO-4-METHOXY-5-NITROTOLUENE
3-Quinolinecarbonitrile,7-ethoxy-4-hydroxy-(9CI)
N-(5-ethoxy-2-methyl-4-nitrophenyl)acetamide
4-Chloro-3-cyano-7-ethoxy-6-nitroquinoline

DownStream

Articles

Sensitivity of Melanoma Cells to EGFR and FGFR Activation but Not Inhibition is Influenced by Oncogenic BRAF and NRAS Mutations.

Pathol. Oncol. Res. 21 , 957-68, (2015)

BRAF and NRAS are the two most frequent oncogenic driver mutations in melanoma and are pivotal components of both the EGF and FGF signaling network. Accordingly, we investigated the effect of BRAF and...

Pelitinib (EKB-569) targets the up-regulation of ABCB1 and ABCG2 induced by hyperthermia to eradicate lung cancer.

Br. J. Pharmacol. 172 , 4089-106, (2015)

Pelitinib is a potent irreversible EGFR TK inhibitor currently in clinical trials for the treatment of lung cancer. Hyperthermia has been applied concomitantly with chemotherapy and radiotherapy to en...

A molecular case report: functional assay of tyrosine kinase inhibitors in cells from a patient's primary renal cell carcinoma.

Cancer Biol. Ther. 14 , 95-9, (2013)

Current therapies for Renal Cell Carcinoma favor vascular endothelial growth factor receptor (VEGF-R) tyrosine kinase (TK) inhibitors (TKIs). In theory, these are most applicable in tumors that have l...

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