BMS-599626
- AC480
- Optical Purity: 99% e.e.
- Soluble in DMSO
- MF: C27H27FN8O3
- MW: 530.55
Description
BMS-599626 is an orally bioavailable, potent and selective EGFR and ErbB2 inhibitor with IC50 values of 22 nM and 32 nM respectively, and inhibits HER4 with reduced potency (IC50 = 190 nM). Inhibits EGFR and ErbB2 with 100-fold greater potency than MEK and Lck. It is an antiproliferative agent in vitro and anti-tumorigenic agent in vivo.
More Information
| Parent CAS No. | 714971-09-2 |
|---|---|
| Chemical Name | (S)-Morpholin-3-ylmethyl 4-(1-(3-fluorobenzyl)-1H-indazol-5-ylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazin-6-ylcarbamate |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | N12C=C(NC(=O)OC[C@H]3NCCOC3)C(C)=C1C(NC1C=CC3N(CC4C=CC=C(F)C=4)N=CC=3C=1)=NC=N2 |&1:8,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C27H27FN8O3/c1-17-23(34-27(37)39-15-22-14-38-8-7-29-22)13-36-25(17)26(30-16-32-36)33-21-5-6-24-19(10-21)11-31-35(24)12-18-3-2-4-20(28)9-18/h2-6,9-11,13,16,22,29H,7-8,12,14-15H2,1H3,(H,34,37)(H,30,32,33)/t22-/m0/s1 |
| InChiKey | LUJZZYWHBDHDQX-QFIPXVFZSA-N |
| CID | 10437018 |
| Short Description | EGFR and ErbB2 inhibitor |
References
- TW Wong et al. Preclinical antitumor activity of BMS-599626, a pan-HER kinase inhibitor that inhibits HER1/HER2 homodimer and heterodimer signaling. Clin Cancer Res. 2006 Oct 15;12(20 Pt 1):6186-93.
- P Haluska et al. HER receptor signaling confers resistance to the insulin-like growth factor-I receptor inhibitor, BMS-536924. Mol Cancer Ther. 2008 Sep;7(9):2589-98.
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