AC480 (BMS-599626) (714971-09-2)

AC480 (BMS-599626) (714971-09-2) Description:

AC480, also known as BMS-599626 is an orally bioavailable inhibitor of the HER1, HER2 and HER4 tyrosine kinases (IC50 =22, 32 and 190 nM, respectively) with potential antineoplastic activity. BMS-599626 inhibits human epidermal growth factor receptors (HER) HER1, HER2 and HER4, thereby inhibiting the proliferation of tumor cells that overexpress these receptors.

AC480 (BMS-599626) (714971-09-2) Specifications:

Product Name	AC480 (BMS-599626)
Chemical Name	BMS-599626; 714971-09-2; AC480; AC-480; BMS 599626; (S)-Morpholin-3-ylmethyl (4-((1-(3-fluorobenzyl)-1H-indazol-5-yl)amino)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl)carbamate
Purity	>98% (HPLC)
CAS Number	714971-09-2
Molecular Formula	C27H27FN8O3
Molecular Weight	530.564 g/mol
Monoisotopic Mass	530.219 g/mol
InChIKey	LUJZZYWHBDHDQX-QFIPXVFZSA-N
InChi Code	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
SMILES	O=C(OC[[email protected]]1NCCOC1)NC2=CN3N=CN=C(NC4=CC5=C(N(CC6=CC=CC(F)=C6)N=C5)C=C4)C3=C2C
Form	Powder
Color	N/A
Solubility	Soluble in DMSO
Storage Temp.	-20°C
Shelf life	>2 years if stored properly
Handling	Protect from air and moisture
Application	an orally bioavailable inhibitor

RIDADR NONH for all modes of transport

References:

HER receptor tyrosine kinase inhibitor, in patients with advanced solid tumors. Soria JC, Cortes J, Massard C, Armand JP, Andreis D, Ropert S, Lopez E, Catteau A, James J, Marier JF, Beliveau M, Martell RE, Baselga J.Ann Oncol. 2019 Jan 9. doi:10.1093/annonc/mdy532. [Epub ahead of print] No abstract available. PMID: 30624604
HER receptor tyrosine kinase inhibitor, in patients with advanced solid tumors. Soria JC, Cortes J, Massard C, Armand JP, De Andreis D, Ropert S, Lopez E, Catteau A, James J, Marier JF, Beliveau M, Martell RE, Baselga J. Ann Oncol. 2012 Feb;23(2):463-71. doi: 10.1093/annonc/mdr137. Epub 2011 May 16. PMID: 21576284
Gavai AV, Fink BE, Fairfax DJ, Martin GS, Rossiter LM, Holst CL, Kim SH, Leavitt KJ, Mastalerz H, Han WC, Norris D, Goyal B, Swaminathan S, Patel B, Mathur A, Vyas DM, Tokarski JS, Yu C, Oppenheimer S, Zhang H, Marathe P, Fargnoli J, Lee FY, Wong TW, Vite GD. Discovery and preclinical evaluation of [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4 ]triazin-6-yl]carbamic acid, (3S)-3-morpholinylmethyl ester (BMS-599626), a selective and orally efficacious inhibitor of human epidermal growth factor receptor 1 and 2 kinases. J Med Chem. 2009 Nov 12;52(21):6527-30. doi: 10.1021/jm9010065. PubMed PMID: 19821562.
Haluska P, Carboni JM, TenEyck C, Attar RM, Hou X, Yu C, Sagar M, Wong TW, Gottardis MM, Erlichman C. 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. doi: 10.1158/1535-7163.MCT-08-0493. Epub 2008 Sep 2. PubMed PMID: 18765823; PubMed Central PMCID: PMC2614316.
Wong TW, Lee FY, Yu C, Luo FR, Oppenheimer S, Zhang H, Smykla RA, Mastalerz H, Fink BE, Hunt JT, Gavai AV, Vite GD. 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. PubMed PMID: 17062696.

HER2&FLT3

AC480 (BMS-599626) (714971-09-2) Description:

AC480 (BMS-599626) (714971-09-2) Specifications:

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