HKI 357

Modify Date: 2025-08-21 21:07:41

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
InChIKey	NERXPXBELDBEPZ-RMKNXTFCSA-N
SMILES	CCOc1cc2ncc(C#N)c(Nc3ccc(OCc4cccc(F)c4)c(Cl)c3)c2cc1NC(=O)C=CCN(C)C

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...

CAS#:99083-25-7

Dimethylamine

CAS#:124-40-3

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

CAS#:848133-14-2

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...

CAS#:214476-09-2

HKI 357

CAS#:848133-17-5

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

CAS#:202197-26-0

HKI 357

CAS#:848133-17-5

HKI 357

L-733,060 hydrochloride

UNII-39R3638KZ6

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HKI 357

Use of HKI 357

Names

HKI 357 Biological Activity

Chemical & Physical Properties

Synthetic Route

Synonyms

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.