BMS-599626
BMS-599626 Basic information
- Product Name:
- BMS-599626
- Synonyms:
-
- [4-[[1-[(3-Fluorophenyl)methyl]-1H-indazol-5-yl]amino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic acid (3S)-3-morpholinylmethyl ester hydrochloride
- BMS-599626 (AC480)
- BMS-599626 (Hydrochloride)
- BMS-599626 HCl
- AC480;BMS-599626 HCL;BMS599626;BMS 599626;AC-480
- BMS-599626 hydrochloride (AC480
- CS-173
- AC480 HCl
- CAS:
- 873837-23-1
- MF:
- C27H28ClFN8O3
- MW:
- 567.0144232
- Mol File:
- 873837-23-1.mol
BMS-599626 Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- ≥29.05 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
- form
- Powder
- color
- White to off-white
BMS-599626 Usage And Synthesis
Uses
BMS-599626 is a highly selective pan-HERKinase inhibitor with IC50 of 20 and 30 nM for the inhibition of HER1and HER2, respectively.
in vivo
BMS-599626 Hydrochloride (60-240 mg/kg; p.o.; daily for 14 days) results in a dose-dependent inhibition of Sal2 tumor growth[1].
BMS-599626 Hydrochloride treatment results in the inhibition of GEO xenograft tumor growth when given once daily for 14 days. In addition to efficacy in the Sal2, GEO, and KPL4 models, BMS-599626 has similar antitumor activity in other HER2 amplified xenograft models including the BT474 breast and N87 gastric tumors, as well as other HER1-overexpressing non-small-cell lung tumors (A549 and L2987)[1].
BMS-599626 Hydrochloride given before and during irradiation improved the radioresponse of HN5 tumors in vivo[2].
| Animal Model: | Athymic female nude mice (nu/nu mice, Sal2 tumor model)[1] |
| Dosage: | 60, 120, 240 mg/kg |
| Administration: | Oral; daily for 14 days |
| Result: | Resulted in a dose-dependent inhibition of Sal2 tumor growth. |
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