BIIB021
Based on 4 publication(s) in Google Scholar
BIIB021 (CNF2024) is an orally active, fully synthetic inhibitor of HSP90 with a Ki and an EC50 of 1.7 nM and 38 nM, respectively.
For research use only. We do not sell to patients.
- Purity: 99.19%
- CAS No.: 848695-25-0
- Formula: C14H15ClN6O
- Molecular Weight:318.76
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) BIIB021
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Biological Activity
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HSP90 1.7 nM (Ki) |
HSP90 38 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 4T1 | IC50 |
0.55 μM
Compound: BIIB021; 13
|
Anticancer activity against mouse 4T1 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Anticancer activity against mouse 4T1 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
|
[PMID: 34864330] |
| A-375 | IC50 |
0.253 μM
Compound: 37; BIIB021
|
Cytotoxicity against human A-375 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Cytotoxicity against human A-375 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
|
[PMID: 36574496] |
| A549 | GI50 |
0.26 μM
Compound: 2; BIIB021
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Antiproliferative activity against human A549 cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay
Antiproliferative activity against human A549 cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay
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[PMID: 33934008] |
| A549 | GI50 |
0.26 μM
Compound: BIIB021
|
Antiproliferative activity against human A549 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human A549 cells measured after 48 hrs by SRB assay
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[PMID: 32683166] |
| A549 | GI50 |
0.33 μM
Compound: 6; BIIB021
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Growth inhibition of human A549 cells incubated for 48 hrs by SRB assay
Growth inhibition of human A549 cells incubated for 48 hrs by SRB assay
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[PMID: 32058238] |
| A549 | GI50 |
0.33 μM
Compound: BIIB021; 6
|
Antiproliferative activity against human A549 cells after 48 hrs by sulforhodamine B assay
Antiproliferative activity against human A549 cells after 48 hrs by sulforhodamine B assay
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[PMID: 29567459] |
| A549 | IC50 |
0.134 μM
Compound: 37; BIIB021
|
Cytotoxicity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Cytotoxicity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
|
[PMID: 36574496] |
| B16-F10 | IC50 |
0.176 μM
Compound: 37; BIIB021
|
Cytotoxicity against mouse B16-F10 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Cytotoxicity against mouse B16-F10 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
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[PMID: 36574496] |
| BT-474 | IC50 |
0.14 μM
Compound: 4, BIIB021
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Binding affinity to Hsp90 nucleotide binding domain in human BT474 cells
Binding affinity to Hsp90 nucleotide binding domain in human BT474 cells
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[PMID: 20608738] |
| HCT-116 | GI50 |
0.15 μM
Compound: BIIB021
|
Antiproliferative activity against human HCT-116 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human HCT-116 cells measured after 48 hrs by SRB assay
|
[PMID: 32683166] |
| HCT-116 | GI50 |
0.15 μM
Compound: BIIB021; 6
|
Antiproliferative activity against human HCT116 cells after 48 hrs by sulforhodamine B assay
Antiproliferative activity against human HCT116 cells after 48 hrs by sulforhodamine B assay
|
[PMID: 29567459] |
| HCT-116 | GI50 |
0.227 μM
Compound: BIIB021
|
Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 30385226] |
| HCT-116 | GI50 |
0.25 μM
Compound: 2; BIIB021
|
Antiproliferative activity against human HCT116 cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay
Antiproliferative activity against human HCT116 cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay
|
[PMID: 33934008] |
| Hep 3B2 | GI50 |
0.24 μM
Compound: 2; BIIB021
|
Antiproliferative activity against human Hep3B cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay
Antiproliferative activity against human Hep3B cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay
|
[PMID: 33934008] |
| HepG2 | IC50 |
0.113 μM
Compound: 37; BIIB021
|
Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
|
[PMID: 36574496] |
| HL-60 | GI50 |
0.59 μM
Compound: BIIB021; 6
|
Antiproliferative activity against human HL60 cells after 48 hrs by sulforhodamine B assay
Antiproliferative activity against human HL60 cells after 48 hrs by sulforhodamine B assay
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[PMID: 29567459] |
| HT-1080 | IC50 |
16.2 μM
Compound: CNF2024; BIIB021
|
Cytotoxicity against human HT-1080 cells incubated for 48 hrs by CCK-8 assay
Cytotoxicity against human HT-1080 cells incubated for 48 hrs by CCK-8 assay
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[PMID: 39230973] |
| HUVEC | GI50 |
1.42 μM
Compound: 2; BIIB021
|
Antiproliferative activity against human HUVEC cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay
Antiproliferative activity against human HUVEC cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay
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[PMID: 33934008] |
| MCF7 | EC50 |
38 nM
Compound: 14, BIIB021
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Inhibition of HSP90alpha in human MCF7 cells assessed as degradation of Her-2
Inhibition of HSP90alpha in human MCF7 cells assessed as degradation of Her-2
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[PMID: 22938030] |
| MCF7 | GI50 |
0.392 μM
Compound: BIIB021
|
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 30385226] |
| MCF7 | IC50 |
1.12 μM
Compound: BIIB021; 13
|
Antiproliferative activity against human MCF-7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human MCF-7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
|
[PMID: 34864330] |
| MCF7 | IC50 |
310 nM
Compound: 17; BIIB021
|
Antiproliferative activity against human MCF7 cells
Antiproliferative activity against human MCF7 cells
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[PMID: 31663736] |
| MCF7 | IC50 |
38 nM
Compound: 6, BIIB021
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Inhibition of HSP90-mediated client protein HER2 degradation in human MCF7 cells
Inhibition of HSP90-mediated client protein HER2 degradation in human MCF7 cells
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[PMID: 20055425] |
| MDA-MB-231 | GI50 |
0.24 μM
Compound: 2; BIIB021
|
Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay
Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay
|
[PMID: 33934008] |
| MDA-MB-231 | IC50 |
0.339 μM
Compound: 37; BIIB021
|
Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
|
[PMID: 36574496] |
| MDA-MB-231 | IC50 |
7.72 μM
Compound: BIIB021; 13
|
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
|
[PMID: 34864330] |
| MDA-MB-468 | IC50 |
2.52 μM
Compound: BIIB021; 13
|
Anticancer activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Anticancer activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
|
[PMID: 34864330] |
| NCI-H1975 | GI50 |
0.2 μM
Compound: 6; BIIB021
|
Growth inhibition of human NCI-H1975 cells incubated for 48 hrs by SRB assay
Growth inhibition of human NCI-H1975 cells incubated for 48 hrs by SRB assay
|
[PMID: 32058238] |
| NCI-H1975 | GI50 |
0.2 μM
Compound: BIIB021
|
Antiproliferative activity against human NCI-H1975 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human NCI-H1975 cells measured after 48 hrs by SRB assay
|
[PMID: 32683166] |
| NCI-H1975 | GI50 |
0.38 μM
Compound: BIIB021; 6
|
Antiproliferative activity against human NCI-H1975 cells after 48 hrs by sulforhodamine B assay
Antiproliferative activity against human NCI-H1975 cells after 48 hrs by sulforhodamine B assay
|
[PMID: 29567459] |
| NCI-H460 | GI50 |
0.21 μM
Compound: BIIB021
|
Antiproliferative activity against human NCI-H460 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human NCI-H460 cells measured after 48 hrs by SRB assay
|
[PMID: 32683166] |
| SK-BR-3 | GI50 |
0.347 μM
Compound: BIIB021
|
Antiproliferative activity against human SK-BR-3 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human SK-BR-3 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 30385226] |
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 enhances the in vitro radiosensitivity of HNSCCA cell lines (UM11B and JHU12) with a corresponding reduction in the expression of key radioresponsive proteins, increases apoptotic cells and enhances G2 arrest[3].BIIB021 is considerably more active than 17-AAG against adrenocortical carcinoma H295R. 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)[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 848695-25-0
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Appearance Solid
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Molecular Weight 318.76
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Formula C14H15ClN6O
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Color White to off-white
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SMILES
ClC1=C2C(N(C=N2)CC3=C(C(OC)=C(C=N3)C)C)=NC(N)=N1
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Synonyms
CNF2024
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Nat Commun
2017 Sep 4;8(1):422. PMID: 28871086 -
Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
Pharmaceuticals (Basel)
Computational Modeling to Identify Drugs Targeting Metastatic Castration-Resistant Prostate Cancer Characterized by Heightened Glycolysis. [Abstract]2024 Apr 29;17(5):569. PMID: 38794139 -
Viruses
Deep Transfer Learning Approach for Automatic Recognition of Drug Toxicity and Inhibition of SARS-CoV-2. [Abstract]2021 Apr 2;13(4):610. PMID: 33918368
Solvent & Solubility
DMSO : ≥ 45 mg/mL (141.17 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.84 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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-
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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 contain no BIIB021 or no Hsp90, respectively. The data are fit to a four-parameter curve and IC50 is generated.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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 viability.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
BALB/c and athymic mice are obtained from Harlan Sprague-Dawley at age 6 to 8 weeks. The mice are maintained in sterilized cages in a ventilated caging system with a 12 h light/12 h dark photoperiod at temperature of 21°C to 23°C and a relative humidity of 50±5%. Irradiated pelleted food and autoclaved deionized water are provided ad libitum. Animals are identified by the use of individually numbered ear tags. N87 tumor fragments (appr 2 mm3) are implanted s.c. in the right flank of the animal. BIIB021 is administered to animals bearing N87 stomach carcinoma tumors at doses of 31, 62.5, and 125 mg/kg, once daily, from Monday to Friday, for 5 weeks. Tumor dimensions are measured using calipers and tumor volumes are calculated using the equation for an ellipsoid sphere (l×w2)/2=mm3, where l and w refer to the larger and smaller dimensions collected at each measurement, respectively. Tumor volumes are measured and animals are weighed and monitored for toxicity at least twice weekly. P values are calculated using the two-tailed Student's t test to assess the difference in tumor volumes between control and treated groups. P<0.05 is considered significant.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (284 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Lundgren, Karen., et al. BIIB021, an orally available, fully synthetic small-molecule inhibitor of the heat shock protein Hsp90. Molecular Cancer Therapeutics (2009), 8(4), 921-929. [Content Brief]
[2]. B?ll B, et al. Heat shock protein 90 inhibitor BIIB021 (CNF2024) depletes NF-kappaB and sensitizes Hodgkin's lymphoma cells for natural killer cell-mediated cytotoxicity. Clin Cancer Res. 2009 Aug 15;15(16):5108-16. [Content Brief]
[3]. Yin X, et al. BIIB021, a novel Hsp90 inhibitor, sensitizes head and neck squamous cell carcinoma to radiotherapy. Int J Cancer. 2010 Mar 1;126(5):1216-25 [Content Brief]
[4]. Zhang H, et al. BIIB021, a synthetic Hsp90 inhibitor, has broad application against tumors with acquired multidrug resistance. Int J Cancer. 2010 Mar 1;126(5):1226-34 [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1372 mL | 15.6858 mL | 31.3716 mL | 78.4289 mL |
| 5 mM | 0.6274 mL | 3.1372 mL | 6.2743 mL | 15.6858 mL | |
| 10 mM | 0.3137 mL | 1.5686 mL | 3.1372 mL | 7.8429 mL | |
| 15 mM | 0.2091 mL | 1.0457 mL | 2.0914 mL | 5.2286 mL | |
| 20 mM | 0.1569 mL | 0.7843 mL | 1.5686 mL | 3.9214 mL | |
| 25 mM | 0.1255 mL | 0.6274 mL | 1.2549 mL | 3.1372 mL | |
| 30 mM | 0.1046 mL | 0.5229 mL | 1.0457 mL | 2.6143 mL | |
| 40 mM | 0.0784 mL | 0.3921 mL | 0.7843 mL | 1.9607 mL | |
| 50 mM | 0.0627 mL | 0.3137 mL | 0.6274 mL | 1.5686 mL | |
| 60 mM | 0.0523 mL | 0.2614 mL | 0.5229 mL | 1.3071 mL | |
| 80 mM | 0.0392 mL | 0.1961 mL | 0.3921 mL | 0.9804 mL | |
| 100 mM | 0.0314 mL | 0.1569 mL | 0.3137 mL | 0.7843 mL |