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HKI-357 (HKI357) is a novel and potent dual inhibitor of EGFR and ERBB2 that irreversibly inhibits EGFR and ERBB2 with IC50s of 34 nM and 33 nM, respectively. HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation.
| ln Vitro |
In NCI-H1975 cells, ligand-induced EGFR autophosphorylation and its downstream signaling are efficiently inhibited by HKI-357 (0.01-10 μM) as shown by AKT and MAPK phosphorylation [1]. In parental NCI-H1650 cells bearing the delE746-A750 EGFR mutation, HKI-357 likewise potently suppresses EGFR autophosphorylation (measured at position Y1068) as well as AKT and MAPK phosphorylation [1].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: NCI-H1975 bronchoalveolar cell line Tested Concentrations: 0.01, 0.01, 0.1, 1 and 10 μM Incubation Duration: Experimental Results: Inhibition of ligand-induced EGFR autophosphorylation and its downstream signals AKT and MAPK phosphorylation change. |
| References | |
| Additional Infomation |
Hki 357 is under investigation in clinical trial NCT00550381 (Study Evaluating the Safety, Tolerability, and Pharmacokinetics (PK) of HKI-357 Administered Orally to Healthy Subjects).
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| Molecular Formula |
C₃₁H₂₉CLFN₅O₃
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|---|---|
| Molecular Weight |
574.05
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| Exact Mass |
573.194
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| Elemental Analysis |
C, 64.86; H, 5.09; Cl, 6.18; F, 3.31; N, 12.20; O, 8.36
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| CAS # |
848133-17-5
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| Related CAS # |
848133-17-5;915942-25-5;
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| PubChem CID |
11238512
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| Appearance |
Off-white to yellow solid powder
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| LogP |
6.747
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
41
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| Complexity |
915
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N(C1C=CC(OCC2C=CC=C(F)C=2)=C(Cl)C=1)C1=C(C#N)C=NC2=CC(=C(C=C12)NC(=O)/C=C/CN(C)C)OCC
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| InChi Key |
NERXPXBELDBEPZ-RMKNXTFCSA-N
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| 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+
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| Chemical Name |
(E)-N-[4-[3-chloro-4-[(3-fluorophenyl)methoxy]anilino]-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide
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| Synonyms |
HKI357 HKI 357
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~174.20 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.36 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (4.36 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.36 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7420 mL | 8.7100 mL | 17.4201 mL | |
| 5 mM | 0.3484 mL | 1.7420 mL | 3.4840 mL | |
| 10 mM | 0.1742 mL | 0.8710 mL | 1.7420 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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