BIIB021

Catalog No.S1175 Synonyms: CNF2024

BIIB021 Chemical Structure

Molecular Weight(MW): 318.76

BIIB021 is an orally available, fully synthetic small-molecule inhibitor of HSP90 with Ki and EC50 of 1.7 nM and 38 nM, respectively. Phase 2.

Size Price Stock Quantity  
USD 120 In stock
USD 210 In stock
USD 420 In stock
USD 770 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

10 Customer Reviews

  • PLoS Pathog 2012 8(11), e1003048. BIIB021 purchased from Selleck.

    PLoS Pathog 2012 8(11), e1003048. BIIB021 purchased from Selleck.

  • (G-I) WST-1 assays of MCF7 (G) with oPRL or 800 nM BIIB021 alone, (H) with DOX ± PRL, or (I) with DOX + BIIB021 ± PRL. n = 18. Data were analyzed with a one-way ANOVA followed by Bonferroni posttests. *P < 0.05; **P < 0.01; ***P < 0.001.

    Endocrinology, 2018, 159(2):907-930. BIIB021 purchased from Selleck.

    Acta Pharmacol Sin 2013 34(12), 1545-53. BIIB021 purchased from Selleck.

  • Acta Pharmacol Sin 2013 34(12), 1545-53. BIIB021 purchased from Selleck.

    Acta Pharmacol Sin 2013 34(12), 1545-53. BIIB021 purchased from Selleck.

  • Acta Pharmacol Sin 2013 34(12), 1545-53. BIIB021 purchased from Selleck.

    Molt-4 cells were cultured with or without varying concentrations of BIIB021 in 96-well plates for 24, 48, and 72 h, respectively. The antiproliferative effects were measured by the MTT assay. BIIB021 effectively inhibited Molt-4 cell growth in a dose- and time-dependent manner.

    Acta Pharmacol Sin 2013 34, 1545-53. BIIB021 purchased from Selleck.

  • The cells were treated with BIIB021 at 100 nmol/L and 200 nmol/L for 24 h and stained with PI. The DNA content was analyzed by flow cytometry.

    Acta Pharmacol Sin 2013 34, 1545-53. BIIB021 purchased from Selleck.

    Molt-4 cells were treated with BIIB021 at the indicated doses for 24 h, and apoptosis was assessed by flow cytometry using Annexin V/PI staining.The results showed that externalized PS, a characteristic of early apoptosis, was increased in the BIIB021-treated Molt-4 cells in a dose-dependent fashion.

    Acta Pharmacol Sin 2013 34, 1545-53. BIIB021 purchased from Selleck.

Purity & Quality Control

Choose Selective HSP (e.g. HSP90) Inhibitors

Biological Activity

Description BIIB021 is an orally available, fully synthetic small-molecule inhibitor of HSP90 with Ki and EC50 of 1.7 nM and 38 nM, respectively. Phase 2.
Targets
HSP90 [1]
(Cell-free assay)
1.7 nM(Ki)
In vitro

BIIB021 binds in the ATP-binding pocket of Hsp90, interferes with Hsp90 chaperone function, and results in client protein degradation and tumor growth inhibition. BIIB021 inhibits tumor cell (BT474, MCF-7, N87, HT29, H1650, H1299, H69 and H82) proliferation with IC50 from 0.06-0.31 μM. BIIB021 induces 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. [1] BIIB021 inhibits Hodgkin's lymphoma cells (KM-H2, L428, L540, L540cy, L591, L1236 and DEV) with IC50 from 0.24-0.8 μM. BIIB021 shows low activity in lymphocytes from healthy individuals. BIIB021 inhibits the constitutive activity of NF-κB despite defective IκB. BIIB021 induces the expression of ligands for the activating NK cell receptor NKG2D on Hodgkin's lymphoma cells resulting in an increased susceptibility to NK cell–mediated killing. [2] BIIB021 enhanced the in vitro radiosensitivity of HNSCCA cell lines (UM11B and JHU12) with a corresponding reduction in the expression of key radioresponsive proteins, increased apoptotic cells and enhance G2 arrest. [3] BIIB021 is considerably more active than 17-AAG against adrenocortical carcinoma H295R, both in vitro and in vivo. The cytotoxic activity of BIIB021 is not influenced by loss of NQO1 or Bcl-2 overexpression, molecular lesions that do not prevent client loss but are nonetheless associated with reduced cell killing by 17-AAG. BIIB021 is also active in 17-AAG resistant cell lines (NIH-H69, MES SA Dx5, NCI-ADR-RES, Nalm6 and etc.). [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
sf9 cells MmPaSpVv[3Srb36gZZN{[Xl? Mme1N{Bp M1TSXmJqdmSrbnegZYZncW6rdImgeI8hcHWvYX6gUk11\XKvaX7hcEBxd2y7SHnzMZRi\2enZDDIV3A6OGKndHGgLGQ6KHSxIFWyN|YqKGW6cILld5Nm\CCrbjDpcpNm[3Ric3[5JINmdGy|IHHmeIVzKDNiaILzJIJ6KG[udX;y[ZNk\W6lZTDwc4xiemm8YYTpc44h[XO|YYmsJGtqRTRibl2= MkHRNlQ{OzJ2OEi=
MCF7 cells NFHo[ZpHfW6ldHnvckBie3OjeR?= M3O3e2lvcGmkaYTpc44hd2ZiSGPQPVBidHCqYTDpckBpfW2jbjDNR2Y4KGOnbHzzJIF{e2W|c3XkJIF{KGSnZ4Lh[IF1cW:wIH;mJGhmei1{LDDFR|UxRTN6IH7N M2PuPFIzQTN6MEOw
human BT474 cells NUC5dpFwTnWwY4Tpc44h[XO|YYm= NWC5XY9SSmmwZHnu[{Bi\m[rbnn0fUB1dyCKc4C5NEBvfWOuZX;0bYRmKGKrbnTpcoch\G:vYXnuJIlvKGi3bXHuJGJVPDd2IHPlcIx{NCCLQ{WwQVAvOTRizszN MUWyNFYxQDd|OB?=
NCI-H1299 cells M2TPcGZ2dmO2aX;uJIF{e2G7 NVzFeWZtOTJiaB?= NWi3TplCWmWmdXP0bY9vKGmwIH;4fYdmdiClb37zeY1xfGmxbjDyZZRmKGmwIHj1cYFvKE6FST3INVI6QSClZXzsd{BqdmO3YnH0[YQh\m:{IEGyJIhzew>? M3TCTVI2Ozh|OUG1

... Click to View More Cell Line Experimental Data

In vivo Oral administration of BIIB021 leads to tumor growth inhibition in many tumor xenograft models including N87, BT474, CWR22, U87, SKOV3 and Panc-1. [1] BIIB021 effectively inhibits growth of L540cy tumor at a dose of 120 mg/kg. [2] BIIB021 significantly enhances antitumor growth effect of radiation in JHU12 xenograft. [3]

Protocol

Kinase Assay:[1]
+ Expand

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:[1]
+ Expand
  • Cell lines: BT474, MCF-7, N87, HT29, H1650, H1299, H69 and H82 cells
  • Concentrations: 3 nM - 1 μM
  • Incubation Time: 5 days
  • Method: 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)
Animal Research:[1]
+ Expand
  • Animal Models: N87, BT474, CWR22, U87, SKOV3 and Panc-1 tumor models in BALB/c and athymic mice
  • Formulation: Phospho-lipon/sucrose emulsion [2]
  • Dosages: 31, 62.5, and 125 mg/kg
  • Administration: Orally administered once daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 64 mg/mL (200.77 mM)
Ethanol 2 mg/mL (6.27 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% propylene glycol, 5% Tween 80, 65% D5W
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 318.76
Formula

C14H15ClN6O

CAS No. 848695-25-0
Storage powder
in solvent
Synonyms CNF2024

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01017198 Completed Advanced Solid Tumors Biogen November 2009 Phase 1
NCT01004081 Completed Breast Cancer Biogen November 2009 Phase 2
NCT00618735 Completed Advanced Solid Tumors Biogen February 2008 Phase 1
NCT00618319 Completed GIST Biogen February 2008 Phase 2
NCT00412412 Completed Breast Cancer Biogen December 2007 Phase 1
NCT00344786 Terminated B-Cell Chronic Lymphocytic Leukemia Biogen February 2006 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

HSP (e.g. HSP90) Signaling Pathway Map

Related HSP (e.g. HSP90) Products

Tags: buy BIIB021 | BIIB021 supplier | purchase BIIB021 | BIIB021 cost | BIIB021 manufacturer | order BIIB021 | BIIB021 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID