XL888 --- HSP90 Inhibitor

Overview
Catalog #	bs-60164c-2mg-solid
Product Name	XL888 --- HSP90 Inhibitor
Specifications
Storage Buffer	Powder
Storage Condition	Store in dry, dark place at -20C for 1 year.
Target
Product Information	Molecular Weight: 503.64 Formula: C29 H37 N5 O3 CAS Number: 1149705-71-4 InChi Key: LHGWWAFKVCIILM-CIQXWFTPSA-N InChi: InChI=1S/C29H37N5O3/c1-4-17(3)32-25-14-23(16(2)11-24(25)28(30)36)29(37)33-20-12-21-8-9-22(13-20)34(21)26-10-7-19(15-31-26)27(35)18-5-6-18/h7,10-11,14-15,17-18,20-22,32H,4-6,8-9,12-13H2,1-3H3,(H2,30,36)(H,33,37)/t17-,20-,21-,22+/m1/s1 Smiles: CC1C=C(C(N)=O)C(=CC=1C(=O)N[C@H]1C[C@@H]2CC[C@H](C1)N2C1C=CC(=CN=1)C(=O)C1CC1)N[C@H](C)CC Purity: 98.0 Solubility: DMSO up to 100 mM Appearance: Solid Power. Shelf Life: 1.0 years
Description	XL888 is a highly potent, ATP-competitive and orally bioavailable small-molecule inhibitor of heat shock protein 90 (Hsp90) with antineoplastic activity. It specifically binds to Hsp90 with an IC50 of 24 nM. XL888 inhibits HSP90’s chaperone function and promotes the proteasomal degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival. In vivo XL888 significantly induces the regression of, or growth inhibition of established M229R and 1205LuR xenografts in SCID mice. XL888 treatment is noted to be proapoptotic in vivo and leads to increased TUNEL staining in M229R xenografts associated with increased expression of BIM and decreased expression of Mcl-1.