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BIIB021

Catalog No. T2286 CAS 848695-25-0

Synonyms: BIIB 021, CNF2024, BIIB-021

BIIB021 (CNF2024) is an orally-available, fully synthetic inhibitor of HSP90(Ki=1.7 nM, EC50=38 nM).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

BIIB021, CAS 848695-25-0

Pack Size	Availability	Price/USD
5 mg	In stock	$ 48.00
10 mg	In stock	$ 68.00
25 mg	In stock	$ 108.00
50 mg	In stock	$ 173.00
100 mg	In stock	$ 263.00
200 mg	In stock	$ 450.00
500 mg	In stock	$ 742.00
1 mL * 10 mM (in DMSO)	In stock	$ 52.00

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Purity: 99.82%

Purity: 98.38%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	BIIB021 (CNF2024) is an orally-available, fully synthetic inhibitor of HSP90(Ki=1.7 nM, EC50=38 nM).
Targets&IC50	HSP90:1.7 nM(Ki)
In vitro	In various transplant tumor models, oral administration of BIIB021 effectively inhibits tumor growth. Specifically, in L540cy tumors, BIIB021 (120 mg/kg) is capable of suppressing cell proliferation.
In vivo	BIIB021 effectively inhibits cell growth in various tumor cell lines (IC50=0.06-0.31 μM), including BT474, MCF-7, N87, HT29, H1650, H1299, H69, and H82. It also suppresses cell proliferation in Hodgkin's lymphoma cells (IC50=0.24-0.8 μM), such as KM-H2, L428, L540, L540cy, L591, L1236, and DEV. Additionally, BIIB021 induces the degradation of Hsp90 proteins (including HER-2, Akt, and Raf-1) and upregulates the expression of heat shock proteins Hsp70 and Hsp27.
Kinase Assay	Hsp90 Binding Assay: For fluorescence polarization competition measurements, the FITC-geldanamycin probe (20 nM) is reduced with 2 mM TCEP at room temperature for 3 hours, after which the solution is aliquoted and stored at -80 °C until used. Recombinant human Hsp90α (0.8 nM) and reduced FITC-geldanamycin (2 nM) are incubated in a 96-well microplate at room temperature for 3 hours in the presence of assay buffer containing 20 mM HEPES (pH 7.4), 50 mM KCl, 5 mM MgCl2, 20 mM Na2MoO4, 2 mM DTT, 0.1 mg/mL BGG, and 0.1% (v/v) CHAPS. Following this preincubation, BIIB021 in 100% DMSO is then added to final concentrations of 0.2 nM to 10 μM (final volume 100 μL, 2% DMSO). The reaction is incubated for 16 hours at room temperature and fluorescence is then measured in an Analyst plate reader, excitation = 485 nm, emission = 535 nm. High and low controls contained no BIIB021 or no Hsp90, respectively. The data are fit to a four-parameter curve and IC50 is generated.
Cell Research	A modified tetrazolium salt assay is used to measure the IC50. Tumor cells are added to 96-well plates and propagated for 24 hours before BIIB021 addition. BIIB021 is added to the plated cells. DMSO (0.03-0.003%) is included as a vehicle control. 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) are 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 gives rise to a soluble formazan product that is secreted into the culture medium. After 4 hours incubation, the formazan product is quantitated spectrophotometrically at a wavelength of 490 nm. Data are acquired using SOFTmaxPRO software, and 100% viability is 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 is calculated from the A490 values as follows: % viability = (A490 nm sample / A490 nm DMSO-treated cells × 100). The IC50 is defined as the concentration that gives rise to 50% inhibition of cell viabilit(Only for Reference)

Synonyms	BIIB 021, CNF2024, BIIB-021
Molecular Weight	318.76
Formula	C14H15ClN6O
CAS No.	848695-25-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 31.9 mg/mL (100 mM)

References and Literature

1. Lundgren K, et al. Mol Cancer Ther, 2009, 8(4), 921-929. 2. Böll B, et al. Clin Cancer Res, 2009, 15(16), 5108-5116. 3. Yin X, et al. Int J Cancer, 2010, 126(5), 1216-1225. 4. Zhang H, et al. Int J Cancer, 2010, 126(5), 1226-1234.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Inhibitor Library Anti-Metabolism Disease Compound Library Anti-Aging Compound Library Bioactive Compounds Library Max Endoplasmic Reticulum Stress Compound Library Bioactive Compound Library

Related Products

Related compounds with same targets

Arimoclomol maleate JG-231 VER49009 HSP70/SIRT2-IN-2 NVP-HSP990 Shepherdin 79-87 acetate Geldanamycin HSP27 inhibitor J2

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

BIIB021 848695-25-0 Autophagy Cytoskeletal Signaling Metabolism HSP BIIB 021 Heat shock proteins CNF2024 inhibit CNF-2024 BIIB-021 CNF 2024 Inhibitor inhibitor

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