HKI 357

Modify Date: 2024-01-15 09:58:42

HKI 357 structure	Common Name	HKI 357
	CAS Number	848133-17-5	Molecular Weight	574.04500
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₃₁H₂₉ClFN₅O₃	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of HKI 357

HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 with IC50s of 34 nM and 33 nM, respectively. HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation[1].

Name	(E)-N-[4-[3-chloro-4-[(3-fluorophenyl)methoxy]anilino]-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide
Synonym	More Synonyms

Description	HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 with IC50s of 34 nM and 33 nM, respectively. HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> JAK/STAT Signaling >> EGFR Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR
Target	EGFR:34 nM (IC50) ErbB2:33 nM (IC50)
In Vitro	HKI-357 (0.01-10 μM) is effective in suppressing ligand-induced EGFR autophosphorylation and its downstream signaling, as determined by AKT and MAPK phosphorylation in NCI-H1975 cells[1]. HKI-357 also is effective in suppressing EGFR autophosphorylation (measured at residue Y1068), and AKT and MAPK phosphorylation in parental NCI-H1650 cells harboring the delE746-A750 EGFR mutation[1]. Western Blot Analysis[1] Cell Line: NCI-H1975 bronchoalveolar cell line Concentration: 0.01, 0.01, 0.1, 1 and 10 μM Incubation Time: Result: Suppressed ligand-induced EGFR autophosphorylation and its downstream signaling AKT and MAPK phosphorylation.
References	[1]. Kwak EL, et al. Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib. Proc Natl Acad Sci U S A. 2005 May 24;102(21):7665-70.

Molecular Formula	C₃₁H₂₉ClFN₅O₃
Molecular Weight	574.04500
Exact Mass	573.19400
PSA	106.23000
LogP	6.74798

4-(4-(3-Fluorob...

CAS#:848133-14-2

~78%

HKI 357

CAS#:848133-17-5

Literature: Wyeth Patent: US2005/59678 A1, 2005 ; Location in patent: Page 4-5 ; US 20050059678 A1

(E)-4-(Dimethyl...

CAS#:1056149-69-9

4-(4-(3-Fluorob...

CAS#:848133-14-2

~81%

HKI 357

CAS#:848133-17-5

Literature: WYETH Patent: WO2005/34955 A1, 2005 ; Location in patent: Page/Page column 13-14 ; WO 2005/034955 A1

4-bromocrotonyl...

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Dimethylamine

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4-(4-(3-Fluorob...

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HKI 357

CAS#:848133-17-5

Literature: Tsou, Hwei-Ru; Overbeek-Klumpers, Elsebe G.; Hallett, William A.; Reich, Marvin F.; Floyd, M. Brawner; Johnson, Bernard D.; Michalak, Ronald S.; Nilakantan, Ramaswamy; Discafani, Carolyn; Golas, Jonathan; Rabindran, Sridhar K.; Shen, Ru; Shi, Xiaoqing; Wang, Yu-Fen; Upeslacis, Janis; Wissner, Allan Journal of Medicinal Chemistry, 2005 , vol. 48, # 4 p. 1107 - 1131

4-Chloro-3-cyan...

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HKI 357

CAS#:848133-17-5

3-Chloro-4-[(3-...

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HKI 357

CAS#:848133-17-5

HKI 357

L-733,060 hydrochloride

UNII-39R3638KZ6

HKI 357

Use of HKI 357

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HKI 357 Biological Activity

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