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Chemical Structure : Neratinib
CAS No.: 698387-09-6
Catalog No.: PC-45813Not For Human Use, Lab Use Only.
Neratinib (HKI-272) is a potent, highly selective, irreversible HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM in cell-free assays.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 50 mg | $128 | In stock | |
| 100 mg | $198 | In stock | |
| 200 mg | Get quote | ||
| 1 g | Get quote |
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Neratinib (HKI-272) is a potent, highly selective, irreversible HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM in cell-free assays.
Neratinib (HKI-272) weakly inhibits KDR and Src (IC50=0.8 and 1.4 uM), no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and c-Met.
Neratinib (HKI-272) inhibits downstream signal transduction events and cell cycle regulatory pathways, leads to arrest at the G(1)-S phase transition, decreases cell proliferation.
Neratinib (HKI-272) is active in HER-2- and EGFR-dependent tumor xenograft models, orally bioavailable.
| M.Wt | 557.0427 | |
| Formula | C30H29ClN6O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
DMSO: 6.4 mg/mL (Need ultrasonic) |
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| Chemical Name/SMILES |
2-Butenamide, N-[4-[[3-chloro-4-(2-pyridinylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-, (2E)- |
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1. Rabindran SK, et al. Cancer Res. 2004 Jun 1;64(11):3958-65.
2. Tsou HR, et al. J Med Chem. 2005 Feb 24;48(4):1107-31.
3. Ji H, et al. Proc Natl Acad Sci U S A. 2006 May 16;103(20):7817-22.
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