Adaphostin

Modify Date: 2024-01-10 19:15:08

Adaphostin structure	Common Name	Adaphostin
	CAS Number	241127-58-2	Molecular Weight	393.47500
	Density	1.33g/cm3	Boiling Point	606.2ºC at 760mmHg
	Molecular Formula	C₂₄H₂₇NO₄	Melting Point	N/A
	MSDS	Chinese USA	Flash Point	320.4ºC

Use of Adaphostin

Adaphostin (NSC 680410), the adamantyl ester of AG957, is a potent p210bcr/abl inhibitor (IC50=14 μM). Adaphostin induces apoptosis in T-lymphoblastic human leukemia cell lines (IC50 ranging from 17 to 216 nM). Adaphostin has significant and selective activity against chronic and acute myeloid leukemia cells. Adaphostin increased the level of reactive oxygen species (ROS) within CLL B cells[1][2][3].

Name	1-adamantyl 4-[(2,5-dihydroxyphenyl)methylamino]benzoate
Synonym	More Synonyms

Description	Adaphostin (NSC 680410), the adamantyl ester of AG957, is a potent p210bcr/abl inhibitor (IC50=14 μM). Adaphostin induces apoptosis in T-lymphoblastic human leukemia cell lines (IC50 ranging from 17 to 216 nM). Adaphostin has significant and selective activity against chronic and acute myeloid leukemia cells. Adaphostin increased the level of reactive oxygen species (ROS) within CLL B cells[1][2][3].
Related Catalog	Signaling Pathways >> Apoptosis >> Apoptosis Research Areas >> Cancer Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Bcr-Abl
In Vitro	Adaphostin down-regulates p210bcr/abl in K562 cells and inhibits granulocyte colony formation in chronic myelogenous leukemia (CML) specimens at lower concentrations without enhanced toxicity in normal progenitors[1]. Adaphostin-induced p53 up-regulation, DNA strand breaks, and ROS production in ML-1 cells is inhibited by N-acetylcysteine (NAC)[4].
References	[1]. Svingen PA, et al. Effects of the bcr/abl kinase inhibitors AG957 and NSC 680410 on chronic myelogenous leukemia cells in vitro. Clin Cancer Res. 2000;6(1):237-249. [2]. Avramis IA, et al. In vitro and in vivo evaluations of the tyrosine kinase inhibitor NSC 680410 against human leukemia and glioblastoma cell lines. Cancer Chemother Pharmacol. 2002;50(6):479-489. [3]. Orsolic N, et al. Adaphostin has significant and selective activity against chronic and acute myeloid leukemia cells. Cancer Sci. 2006;97(9):952-960. [4]. Chandra J, et al. Involvement of reactive oxygen species in adaphostin-induced cytotoxicity in human leukemia cells. Blood. 2003;102(13):4512-4519.

Density	1.33g/cm3
Boiling Point	606.2ºC at 760mmHg
Molecular Formula	C₂₄H₂₇NO₄
Molecular Weight	393.47500
Flash Point	320.4ºC
Exact Mass	393.19400
PSA	70.00000
LogP	4.99130
Vapour Pressure	2.73E-15mmHg at 25°C
Index of Refraction	1.661