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BIIB021

Cat. No. M1679
BIIB021 Structure
Synonym:

CNF2024

Size Price Availability Quantity
10mg USD 80 In stock
50mg USD 210 In stock
100mg USD 320 In stock
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Quality Control
Biological Activity

BIIB021 (CNF2024) is an orally available synthetic non-ansamycin Hsp90 inhibitor with ki value of 1.7nM. BIIB021 (CNF2024) selectively and potently inhibits the molecular chaperone Hsp90 thereby inhibiting the proper assembly of multiple oncogenic proteins involved in tumor growth and survival.BIIB021 (CNF2024) has antitumor activity in Hodgkin's lymphoma in vitro and in vivo. BIIB021 (CNF2024) selectively induced Hodgkin's lymphoma cell death but did not kill normal lymphocytes from healthy individuals. BIIB021 inhibited the activity of NF-κB, which was independent of IκB mutations.

Protocol
Cell Experiment
Cell lines N87, MCF-7 and BT474 cell lines
Preparation method Cell Proliferation Assay.
A modified tetrazolium salt assay was used to measure the inhibition of tumor cell growth. Cells were added to 96-well plates and propagated for 24 h before compound addition. The compound was serially diluted and added at a concentration range of 3 to 1,000 nmol/L to the plated cells. DMSO (0.03-0.003%) was included as a vehicle control. Cells were incubated in the presence of compound for 5 days. After incubation phenazine methosulfate (stock concentration 1 mg/mL) and 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium, inner salt (stock concentration 2 mg/mL; Promega) were mixed at a ratio of 1:20 and added to each well of a 96-well plate. Reduction of 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium, inner salt gave rise to a soluble formazan product that was secreted into the culture medium. After 4 h incubation, the formazan product was quantitated spectrophotometrically at a wavelength of 490 nm. Data were acquired using SOFTmaxPRO software, and 100% viability was defined as the A490 of DMSO-treated cells stained with 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium, inner salt (the mean A490 of cells treated with DMSO at a range of 0.03-0.003%). Percent viability of each sample was calculated from the A490 values as follows: % viability = (A490 nm sample / A490 nm DMSO-treated cells × 100). The IC50 was defined as the concentration that gave rise to 50% inhibition of cell viability.
Concentrations 3 ~ 1000 nM
Incubation time 5 days
Animal Experiment
Animal models nude mice bearing N87 stomach carcinoma tumors xenograft model
Formulation
Dosages 31, 62.5, and 125 mg/kg, once daily, from Monday to Friday, for 5 weeks
Administration orally
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 318.76
Formula C14H15ClN6O
CAS Number 848695-25-0
Purity 100.00%
Solubility DMSO
Storage at -20°C
References

Phase II study of the HSP90-inhibitor BIIB021 in gastrointestinal stromal tumors.
Dickson et al. Ann Oncol. 2012 Aug 16. PMID: 22898035.

In vitro metabolism of BIIB021, an inhibitor of heat shock protein 90, in liver microsomes and hepatocytes of rats, dogs, and humans and recombinant human cytochrome P450 isoforms.
Xu et al. Drug Metab Dispos. 2012 Apr;40(4):680-93. PMID: 22217465.

An investigation into the potential use of serum Hsp70 as a novel tumour biomarker for Hsp90 inhibitors.
Dakappagari et al. Biomarkers. 2010 Feb;15(1):31-8. PMID: 19747088.

BIIB021, a synthetic Hsp90 inhibitor, has broad application against tumors with acquired multidrug resistance.
Zhang et al. Int J Cancer. 2010 Mar 1;126(5):1226-34. PMID: 19676042.

BIIB021, an orally available, fully synthetic small-molecule inhibitor of the heat shock protein Hsp90.
Lundgren K, et al. Mol Cancer Ther. 2009 Apr;8(4):921-9. PMID: 19372565.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: BIIB021, CNF2024 supplier, HSP90, inhibitors

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