Adaphostin

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

Adaphostin Structure
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].

 Names

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

 Adaphostin Biological Activity

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
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.

 Chemical & Physical Properties

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

 Safety Information

RIDADR NONH for all modes of transport

 Synonyms

tyrphostin AG957 adamantyl ester
4'-adamantylbenzoate-1'-N-1,4-dihydroxybenzylamine
AG 957,Adamantyl Ester
Adaphostin
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