Research Area
Product Type
United States ( Change Country )
BIIB021 Chemical Structure
Elesclomol
HSP-70 Inducer
AUY922 (NVP-AUY922)
NVP-AUY922 (VER-52296) is a highly potent HSP90 inhibitor to HSP90α and HSP90β with IC50 of 13 nM and 21 nM, respectively.
17-AAG (Geldanamycin)
17-AAG (Geldanamycin) is a less toxic analogue of the geldanamycin which binds to Hsp90 and alters its function.
17-DMAG HCl (Alvespimycin)
17-DMAG HCl (Alvespimycin) is a selective Hsp90 inhibitor with a GI50 of 53 nM.
Ganetespib (STA-9090)
Ganetespib is a unique triazolone-containing Hsp90 inhibitor with an IC50 of 4 nM for OSA 8 cells.
AT13387
AT13387 is a selective potent small molecule heat shock protein 90 (Hsp90) inhibitor for A375, MV4-11, NCI-H1975 and SKBr3 cell lines with IC50 of 18 nM, 12 nM, 22 nM and 55 nM, respectively.
MPC-3100
MPC-3100 is a fully synthetic potent small-molecule Hsp90 inhibitor with an IC50 of 60 nM.
NVP-BEP800
NVP-BEP800 is a novel, fully synthetic, oral Hsp90 inhibitor with an IC50 of 0.058 ± 0.006 μM.
SNX-2112
SNX-2112 is a potent synthetic heat shock protein 90 inhibitor with an IC50 of 0.92 μM for K562 cells.
PF-04929113 (SNX-5422)
PF-04929113 (SNX-5422) is a potent and selective Hsp90 inhibitor with an IC50 of median 50 nM.
Biological Activity
BIIB021,formerly CNF2024,is a novel fully synthetic inhibitor of Hsp90. It binds competitively with geldanamycin in the ATP-binding pocket of Hsp90 (Ki=1.7nM). [1]In tumor cells, BIIB021 induced the degradation of Hsp90 client proteins (including HER-2, AKT, and Raf-1) and up-regulated expression of the heat shock proteins Hsp70 and Hsp27. BIIB021 inhibits cell growth and death in variety cell lines (breast, colon, lung) at nanomolar concentrations (IC50: 60nM-250nM) [1] .
Oral administration of BIIB021 led to the inhibition of tumor growth in several human tumor xenograft models. BIIB021 is currently in phase I and II clinical trials in hematopoietic malignancies and solid tumors. [1]
References on BIIB021
- [1] Karen Lundgren, Hong Zhang,et al. 2009;8:921-929
Product Information
| Molecular Weight (WM): | 318.76 |
|---|---|
| Formula: | C14H15ClN6O |
| CAS No.: | 848695-25-0 |
| Synonyms: |
CNF2024
|
| Dissolve in (25°C): | DMSO ≥64mg/mL |
| Water <1mg/mL | |
| Ethanol ≥2mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
Research Area
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