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PZ0197

Pelitinib

≥98% (HPLC)

Synonym(s):

(2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide, EKB 569, EKB-569, WAY-EKB-569

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About This Item

Empirical Formula (Hill Notation):
C24H23ClFN5O2
CAS Number:
257933-82-7
Molecular Weight:
467.92
UNSPSC Code:
51111800
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
powder
Storage condition:
desiccated, protect from light
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Quality Segment

100

assay

≥98% (HPLC)

form

powder

storage condition

desiccated, protect from light

color

white to beige

solubility

DMSO: 5 mg/mL, clear (warmed)

storage temp.

−20°C

SMILES string

Fc1c(cc(cc1)Nc2c3c(ncc2C#N)cc(c(c3)NC(=O)\C=C\CN(C)C)OCC)Cl

InChI

1S/C24H23ClFN5O2/c1-4-33-22-12-20-17(11-21(22)30-23(32)6-5-9-31(2)3)24(15(13-27)14-28-20)29-16-7-8-19(26)18(25)10-16/h5-8,10-12,14H,4,9H2,1-3H3,(H,28,29)(H,30,32)/b6-5+

InChI key

WVUNYSQLFKLYNI-AATRIKPKSA-N

Biochem/physiol Actions

Pelitinib specifically targets cancer cells with elevated expression of the efflux transporters ATP-binding cassette (ABC)B1/ABCG2 post hyperthermia. This property of peltinib aids in the elimination of metastasis and prevention of cancer recurrence.
Pelitinib (EKB-569) is an orally active, potent, second generation irreversible epidermal growth factor receptor tyrosine kinase (EGFR TK) inhibitor. Pelitinib is selective for EGFR (ErbB-1) with an IC50 about 80 nM, but also covalently binds to ErbB-2 (HER2/c-neu) and ErbB-4 (Her 4) with much lower potency. Pelitinib has been shown to inhibit the growth of EGFR-overexpressing tumor cell lines.

Other Notes

Light sensitive

pictograms

Skull and crossbones
GHS06

signalword

Danger

hcodes

H301

Hazard Classifications

Acute Tox. 3 Oral

Storage Class

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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