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Neratinib (HKI-272) HER2/EGFR Inhibitor

Cat.No.S2150

Neratinib is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM in cell-free assays; weakly inhibits KDR and Src, no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and c-Met. Phase 3.

Neratinib (HKI-272) HER2 inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 557.04

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Quality Control

Batch: Purity: 99.94%

99.94

Related Targets	EGFR VEGFR FGFR PDGFR c-Met Src MEK CSF-1R FLT3 c-Kit
Other HER2 Inhibitors	Sevabertinib (BAY 2927088) CP-724714 Sapitinib (AZD8931) Mubritinib (TAK 165) AC480 (BMS-599626) Tyrphostin AG 879 HER2-Inhibitor-1 Zongertinib (BI 1810631) TAS0728 IAM1363

Solubility in DMSO or Water

In vitro
Batch:

DMSO : 6 mg/mL (10.77 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 7 mg/mL (12.56 mM) Warmed with 60°C water bath; Ultrasonicated;
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 2 mg/mL (3.59 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 3 mg/mL (5.38 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 5 mg/mL (8.97 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

The solubility data above are all experimental results (not literature values).

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	30%PEG400 1 0.5%Tween80 2 5%propylene glycol Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (8.98mM)	Taking the 1 mL working solution as an example, add 300 μL of 16.67 mg/ml clarified PEG400 stock solution to 5 μL of Tween80, mix evenly to clarify it; add 50 μL Propylene glycol to the above system, mix evenly to clarify it; then continue to add 645 μL ddH2O Dilute to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Read more about Neratinib (HKI-272) solubility in DMSO or water

Search directly for a cell line, or select a cell line to find matched working concentrations

Read more about Neratinib (HKI-272) working concentrations for cell culture treatment

Neratinib (HKI-272) is a potent inhibitor of HER2 kinase (5.6 nmol/L), EGFR kinase (92 nM), MST1 (37.7 nM), EGFR (81 ± 9 nM), MAP4K4 (33.48 nM), MST2 (87.81 nM), HER2 (2–3 nM), HER4 (19 nM), BT474 (6.7 nM), EFM-192A (46.7 nM), UACC-812 (<5 nM), MDA-MB-361 (7.36 ± 2.65 nM), HCC1419 (3.94 ± 0.5 nM), HCC1569 (<5 nM), HCC1954 (325 nM), JIMT-1 (141.5 ± 9.61 nM), MDA-MB-453 (267.23 ± 22.52 nM), SKBR3 (10.2 nM), SUM-190 (10 ± 0.0 nM), SUM-225 (10 ± 0.0 nM), UACC-732 (650 ± 370 nM), UACC-893 (<5 nM), MCF7 (>3000 nM), T47D (890 nM), HCC1937 (750 nM), SUM-229PE (14 nM), MDA-MB-231 (496 ± 98 nM), MDA-MB-468 (36 nM), MCF10A HER2 WT (<2480 ± 50 nM), MCF10A G309A (<2470 ± 50 nM), MCF10A V777L (<21040 ± 570 nM), MCF10A D769H (<2980 ± 950 nM), MCF10A V842I (<2650 ± 210 nM), MCF10A del.755–759 (2.1 ± 0.2 nM), MCF10A L755S (15.6 ± 6 nM), MCF10A K75E (32 ± 8 nM), MCF10A L768S (<21050 ± 480 nM), MCF10A V773L (<2960 ± 380 nM), MCF10A R647K (<2650 ± 370 nM), MCF10A I655V (<2520 ± 420 nM), MCF10A K676R (<2385 ± 270 nM), MCF10A Q680R (<2550 ± 190 nM), MEK1, MEK2, P-gp, EGFR Cys-797, EGFR T790M, HER2 P780_Y781insGSP, HER2 K753E, HER2 L755S, HER2 D769Y, PIK3CA, PD-1, membrane-bound ATP transporter. Neratinib (HKI-272) exhibits the greatest inhibitory potency toward HER2 (IC50 = 2–3 nM).

Read more about selectivity & specificity

Mechanism of Action

Information	Neratinib (HKI-272) is a potent, irreversible pan-HER and MST1 inhibitor. It affects EGFR/HER2, PI3K/AKT, and MAPK signaling by irreversibly binding to HER kinases and blocking downstream pathways, effectively inhibiting cancer cell proliferation and inducing apoptosis.
Read more about Neratinib (HKI-272) IC50 for cell-based and cell-free assays
Primary Applications and Mechanism of Action

Read more about Neratinib (HKI-272) Mechanism of Action

Chemical Information, Storage & Stability

Molecular Weight	557.04	Formula	C₃₀H₂₉ClN₆O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	698387-09-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	HKI-272			Smiles	CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)OCC4=CC=CC=N4)Cl)C#N)NC(=O)C=CCN(C)C

Read more about storage & stability

Read more comparative analysis about Neratinib (HKI-272)

Tech Support

Handling Instructions

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Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions

Concentration (start):

Dilution-folds:

Computed Result

C1=C0/X	C1:		LOG(C1):
C2=C1/X	C2:		LOG(C2):
C3=C2/X	C3:		LOG(C3):
C4=C3/X	C4:		LOG(C4):
C5=C4/X	C5:		LOG(C5):
C6=C5/X	C6:		LOG(C6):
C7=C6/X	C7:		LOG(C7):
C8=C7/X	C8:		LOG(C8):