HKI-357
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MedKoo CAT#: 462306

CAS#: 848133-17-5 (free base)

Description: HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2. HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation.


Chemical Structure

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HKI-357
CAS# 848133-17-5 (free base)

Theoretical Analysis

MedKoo Cat#: 462306
Name: HKI-357
CAS#: 848133-17-5 (free base)
Chemical Formula: C31H29ClFN5O3
Exact Mass: 573.19
Molecular Weight: 574.053
Elemental Analysis: C, 64.86; H, 5.09; Cl, 6.18; F, 3.31; N, 12.20; O, 8.36

Price and Availability

Size Price Availability Quantity
50mg USD 950 2 Weeks
100mg USD 1650 2 Weeks
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Related CAS #: 848133-17-5 (free base)   915942-25-5 (maleate)    

Synonym: HKI-357; HKI357; HKI 357

IUPAC/Chemical Name: (E)-N-(4-((3-chloro-4-((3-fluorobenzyl)oxy)phenyl)amino)-3-cyano-7-ethoxyquinolin-6-yl)-4-(dimethylamino)but-2-enamide

InChi Key: NERXPXBELDBEPZ-RMKNXTFCSA-N

InChi Code: InChI=1S/C31H29ClFN5O3/c1-4-40-29-16-26-24(15-27(29)37-30(39)9-6-12-38(2)3)31(21(17-34)18-35-26)36-23-10-11-28(25(32)14-23)41-19-20-7-5-8-22(33)13-20/h5-11,13-16,18H,4,12,19H2,1-3H3,(H,35,36)(H,37,39)/b9-6+

SMILES Code: O=C(NC1=C(OCC)C=C2N=CC(C#N)=C(NC3=CC=C(OCC4=CC=CC(F)=C4)C(Cl)=C3)C2=C1)/C=C/CN(C)C

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 574.05 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Kwak EL, Sordella R, Bell DW, et al. Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib. Proc Natl Acad Sci U S A. 2005;102(21):7665-7670. doi:10.1073/pnas.0502860102