NERATINIB MALEATE
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 1g | $450 | Check With Us |
| 5g | $1150 | Check With Us |
| 10g | $1725 | Check With Us |
: Cat #: V3916 CAS #: 915942-22-2 Purity ≥ 98%
Description: Neratinib maleate, the maleate salt of neratinib (HKI-272; PB-272; Nerlynx), is an orally bioavailable HER2 and EGFR inhibitor approved by FDA in 2017 to reduce the risk of breast cancer returning.
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- Physicochemical and Storage Information
- Protocol
- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 673.11 |
|---|---|
| Molecular Formula | C30H29ClN6O3. C4H4O4 |
| CAS No. | 915942-22-2 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: > 10 mMr |
| Water: <1 mg/mLr | |
| Ethanol: <1 mg/mL | |
| Solubility In Vivo | 30% PEG400+0.5% Tween80+5% propylene glycol: 5 mg/mL |
| SMILES Code | O=C(NC1=C(OCC)C=C2N=CC(C#N)=C(NC3=CC=C(OCC4=NC=CC=C4)C(Cl)=C3)C2=C1)/C=C/CN(C)C.O=C(O)/C=CC(O)=O |
| Synonyms | HKI-272 maleate or PB272; HKI272; HKI 272; PB 272; PB-272 maleate |
| Protocol | In Vitro | Neratinib results in the inhibition of MAPK and Akt phosphorylation, down-regulation of cyclin D1 levels, and induction of p27. Neratinib (0-2 nM, 12-16 h) arrests BT474 cell cycle at G1-S phase. Neratinib (0.5 ng/mL–5 μg/mL, 2 days) inhibits the proliferation of cell lines that show high levels of HER-2 (3T3/neu, SK-Br-3, and BT474) and is much less active in cell lines that express neither HER-2 nor EGFR (3T3, MDA-MB-435, and SW620) . Neratinib displays no activity against other serine-threonine kinases such as Akt, cyclin D1/cdk4, cyclin E/cdk2, cyclin B1/cdk1, IKK-2, MK-2, PDK1, c-Raf, and Tpl-2, as well as the tyrosine kinase c-Met. |
|---|---|---|
| In Vivo | Neratinib (HKI-272) (0-80 mg/kg/day; i.g.; 42 days) shows anticancer activities against cancer cells that expresses high levels of HER-2 or EGFR. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 1.4856 mL | 7.4282 mL | 14.8564 mL | 29.7128 mL |
| 5mM | 0.2971 mL | 1.4856 mL | 2.9713 mL | 5.9426 mL |
| 10mM | 0.1486 mL | 0.7428 mL | 1.4856 mL | 2.9713 mL |
| 20mM | 0.0743 mL | 0.3714 mL | 0.7428 mL | 1.4856 mL |
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
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Volume
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Molecular Weight*
The dilution calculator equation
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Volume(start)
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This equation is commonly abbreviated as: C1 V1 = C2 V2
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Step One: Enter information below
Dosage mg/kg
Average weight of animals g
Dosing volume per animal µL
Number of animals
Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
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 add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (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.