HKI 357|cas 848133-17-5

Cas No.:	848133-17-5
Chemical Name:	HKI-357
Synonyms:	HKI 357
SMILES:	O=C(/C=C/CN(C)C)N([H])C1=C(OCC)C=C(N=CC(C#N)=C2N([H])C3=CC=C(OCC4=CC=CC(F)=C4)C(Cl)=C3)C2=C1
Formula:	C₃₁H₂₉ClFN₅O₃
M.Wt:	574.053
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

HKI 357 is an irreversible dual inhibitor of the EGF receptor tyrosine kinases EGFR and HER2 (IC50s = 34 and 33 nM, respectively). It inhibits proliferation of A431, SK-BR-3, and SW620 cancer cell lines (IC50s = 120, 2.5, and 511 nM, respectively). HKI 357 suppresses EGFR autophosphorylation and phosphorylation of the downstream effectors AKT and ERK in the gefitinib-susceptible and -resistant cell lines NCI-H1650 and NCI-H1650(G7), respectively.In vivo, HKI 357 (10 mg/kg) inhibits tumor growth in BT474, A431, and SUM190 mouse xenograft models.

Cat. No.	Product name	Field of application
DC47669	EGFR-IN-18	EGFR-IN-18 potently inhibits enzymatic activity in L858R/T790M/C797S mutant EGFR (4.9 nM), with a significantly lower activity for wild-type EGFR (47 nM).
DC47668	EGFR-IN-17	EGFR-IN-17 is a potent and selective inhibitor of the epidermal growth factor receptor ( IC50 0.0002 μM) to overcome C797S-mediated resistance.
DC47667	EGFR/CSC-IN-1	EGFR/CSC-IN-1 is a potential EGFR (IC50 10.52 nM) and cancer stem cell (CSC) dual inhibitor for triple-negative breast cancer treatment.
DC47271	Tyrphostin 8	Tyrphostin 8 is a tyrosine kinase, with an IC50 of 560 μM for EGFR kinase. Tyrphostin 8 is also a GTPase inhibitor. Tyrphostin 8 can inhibit the protein serine/threonine phosphatase calcineurin (IC50=21 μM).
DC47115	Befotertinib	Befotertinib (D-0316) is the third-generation EGFR tyrosine kinase inhibitor. Befotertinib can be used for the research of EGFR T790M-positive non-small cell lung cancer (NSCLC).
DC46929	Erlotinib-13C6	Erlotinib-13C6 (CP-358774-13C6) is a 13C-labeled Erlotinib. Erlotinib is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR.
DC46464	BGB-102	BGB-102 is a potent multi-kinase inhibitor against EGFR, HER2, and HER4 with IC50s of 9.6 nM, 18 nM and 40.3 nM, respectively.
DC46456	JNJ28871063 hydrochloride	JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC50 values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2.
DC46434	JBJ-02-112-05	JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 15 nM for EGFRL858R/T790M.
DC46219	EGFR mutant-IN-1	EGFR mutant-IN-1, a 5-methylpyrimidopyridone derivative, is a potent and selective EGFRL858R/T790M/C797S mutant inhibitor with an IC50 of 27.5 nM, while being a significantly less potent for EGFRWT (IC50 >1.0 μM).