Neratinib
| Code | Size | Price |
|---|
| CDX-N0326-M050 | 50 mg | £108.00 |
Quantity:
| CDX-N0326-M100 | 100 mg | £157.00 |
Quantity:
| CDX-N0326-M250 | 250 mg | £304.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
AMBIENT
Storage:
Short Term: +4°C Long Term: -20°C
Documents
Further Information
Alternate Names/Synonyms:
HKI-272
Appearance:
Off-white powder.
CAS:
698387-09-6
EClass:
32160000
Form (Short):
liquid
GHS Symbol:
GHS08
Handling Advice:
Protect from light and moisture.
Hazards:
H225+H302+H332, H312, H319
InChi:
InChI=1S/C30H29ClN6O3/c1-4-39-28-16-25-23(15-26(28)36-29(38)9-7-13-37(2)3)30(20(17-32)18-34-25)35-21-10-11-27(24(31)14-21)40-19-22-8-5-6-12-33-22/h5-12,14-16,18H,4,13,19H2,1-3H3,(H,34,35)(H,36,38)/b9-7+
InChiKey:
JWNPDZNEKVCWMY-VQHVLOKHSA-N
Long Description:
Chemical. CAS: 698387-09-6. Formula: C30H29ClN6O3. MW: 557. Neratinib is a cell-permable, irreversible, selective inhibitor of the HER2 kinase (IC50=59nM) and EGFR (IC50=92nM) by preventing phosphorylation of these proteins by their respective kinases. It also potently inhibits several mutants of HER2 and shows 10-fold or greater selectivity over a wide variety of other kinases. As an irreversible inhibitor, neratinib may circumvent acquired resistance developed against reversible inhibitors, including gefitinib. Neratinib displays activity against a variety of cancer cell lines, including A431, 3T3, and MDA-MB-435. Neratinib has been evaluated in clinical trials against cancers characterized by HER2 overexpression or HER2 activating mutations.
MDL:
MFCD09752958
Molecular Formula:
C30H29ClN6O3
Molecular Weight:
557
Package Type:
Vial
Precautions:
P201, P202, P281, P308+313
Product Description:
Neratinib is a cell-permable, irreversible, selective inhibitor of the HER2 kinase (IC50=59nM) and EGFR (IC50=92nM) by preventing phosphorylation of these proteins by their respective kinases. It also potently inhibits several mutants of HER2 and shows 10-fold or greater selectivity over a wide variety of other kinases. As an irreversible inhibitor, neratinib may circumvent acquired resistance developed against reversible inhibitors, including gefitinib. Neratinib displays activity against a variety of cancer cell lines, including A431, 3T3, and MDA-MB-435. Neratinib has been evaluated in clinical trials against cancers characterized by HER2 overexpression or HER2 activating mutations.
Purity:
>98%
Signal word:
Warning
SMILES:
CCOC1=C(NC(/C=C/CN(C)C)=O)C=C(C(NC2=CC(Cl)=C(OCC3=NC=CC=C3)C=C2)=C(C#N)C=N4)C4=C1
Solubility Chemicals:
Soluble in DMSO (2mg/ml). Insoluble in water.
Transportation:
Non-hazardous
UNSPSC Category:
Biochemical Reagents
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.
References
(1) S.K. Rabindran, et al.; Cancer Res. 64, 3958 (2004) | (2) E.L. Kwak, et al.; PNAS 102, 7665 (2005) | (3) H. Ji, et al.; PNAS 103, 7817 (2006) | (4) P. Bose & H. Ozer; Expert. Opin. Investig. Drugs 18, 1735 (2009) (Review) | (5) M.I. Davis, et al.; Nat. Biotechnol. 29, 1046 (2011) | (6) S.M. Kavuri, et al.; Cancer Discov. 5, 832 (2015) | (7) M. Segovia-Mendoza, et al.; Am. J. Cancer Res. 5, 2531 (2015) | (8) S.R. Tiwari, et al.; Clin. Breast Cancer 16, 344 (2016) (Review)