2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. 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.

For research use only. We do not sell to patients.

HKI-357 Chemical Structure

HKI-357 Chemical Structure

CAS No. : 848133-17-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 197 In-stock
Solution
10 mM * 1 mL in DMSO USD 197 In-stock
Solid
1 mg USD 70 In-stock
5 mg USD 156 In-stock
10 mg USD 250 In-stock
25 mg USD 475 In-stock
50 mg USD 689 In-stock
100 mg USD 1000 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of HKI-357:

HKI-357 Related Antibodies

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

IC50 & Target[1]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

HKI-357 Related Antibodies

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.
Clinical Trial
Molecular Weight

574.05

Formula

C31H29ClFN5O3
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (174.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.36 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (4.36 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.65%

SDS (251 KB)

COA (253 KB) HNMR (295 KB) LCMS (255 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7420 mL 8.7100 mL 17.4201 mL 43.5502 mL
5 mM 0.3484 mL 1.7420 mL 3.4840 mL 8.7100 mL
10 mM 0.1742 mL 0.8710 mL 1.7420 mL 4.3550 mL
15 mM 0.1161 mL 0.5807 mL 1.1613 mL 2.9033 mL
20 mM 0.0871 mL 0.4355 mL 0.8710 mL 2.1775 mL
25 mM 0.0697 mL 0.3484 mL 0.6968 mL 1.7420 mL
30 mM 0.0581 mL 0.2903 mL 0.5807 mL 1.4517 mL
40 mM 0.0436 mL 0.2178 mL 0.4355 mL 1.0888 mL
50 mM 0.0348 mL 0.1742 mL 0.3484 mL 0.8710 mL
60 mM 0.0290 mL 0.1452 mL 0.2903 mL 0.7258 mL
80 mM 0.0218 mL 0.1089 mL 0.2178 mL 0.5444 mL
100 mM 0.0174 mL 0.0871 mL 0.1742 mL 0.4355 mL
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HKI-357 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HKI-357848133-17-5HKI357HKI 357EGFREpidermal growth factor receptorErbB-1HER1ERBB2NSCLCsInhibitorinhibitorinhibit

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