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].

Product Specifications

CAS Number

[241127-58-2]

Product Name Alternative

NSC 680410

UNSPSC

12352005

Hazard Statement

H302, H315, H319

Target

Apoptosis; Bcr-Abl

Type

Reference compound

Related Pathways

Apoptosis; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/adaphostin.html

Purity

99.02

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

O=C(C(C=C1)=CC=C1NCC(C=C2O)=C(C=C2)O)OC3(C[C@H](C4)C5)C[C@H]5C[C@H]4C3

Molecular Formula

C24H27NO4

Molecular Weight

393.48

Precautions

H302, H315, H319

References & Citations

[1]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. |[2]Orsolic N, et al. Adaphostin has significant and selective activity against chronic and acute myeloid leukemia cells. Cancer Sci. 2006;97 (9) :952-960. |[3]Chandra J, et al. Involvement of reactive oxygen species in adaphostin-induced cytotoxicity in human leukemia cells. Blood. 2003;102 (13) :4512-4519. |[4]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.