AG 957, Adamantyl Ester

Application:	An ~3-4 fold more potent derivative of AG 957
Molecular Weight:	393.5
Molecular Formula:	C₂₄H₂₇NO₄

Description

AG 957, Adamantyl Ester is a lipophilic, adamantyl ester form of tyrphostin AG 957 that displays anti-proliferative properties. The product has been shown to be selective and is ~3-4 fold more potent than the bcr/abl kinase inhibitor AG 957. AG 957, Adamantyl Ester Downregulates p210bcr/abl autokinase activity (IC₅₀ = 14 µM). Selectively blocks granulocyte colony formation in CML (chronic myelogenous leukemia) progenitors and inhibits proliferation of K562 cells (IC₅₀ = 9.8 µM) by inducing apoptosis. AG 957, Adamantyl Ester is reported to retain activity in STI571-resistant and p53-null human leukemia cell lines (IC₅₀ ~0.1-0.25 µM).

Technical Information

Appearance:	White
Physical State:	Solid
Solubility:	DMSO or EtOH
Storage:	Store at -20° C

Safety and Reference Information

PubChem CID:	387042
SMILES:	C1C2CC3CC1CC(C2)(C3)OC(=O)C4=CC=C(C=C4)NCC5=C(C=CC(=C5)O)O

For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.

References

Avramis, I.A., et al. 2002. Cancer Chemother. Pharmacol. 50, 479. Mow, B.M., et al. 2002. Blood 99, 664. Svingen, P.A., et al. 2000. Clin. Cancer Res. 6, 237.

SDS

Datasheet/SDS