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BIIB021

SKU: orb1305792

Description

BIIB021 (CNF2024) is a potent, fully synthetic, and orally bioavailable HSP90 inhibitor with a Ki of 1.7 nM and an EC50 of 38 nM. This small molecule is a valuable research tool for studying HSP90's role in oncology and neurodegenerative diseases, demonstrating activity in both cellular and animal models of cancer.

Research Area

Cell Biology, Metabolism Research, Signal Transduction

Images & Validation

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BIIB021

Key Properties

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CAS Number848695-25-0
MW318.76
Purity99.82% (May vary between batches)
FormulaC14H15ClN6O
SMILESCOc1c(C)cnc(Cn2cnc3c(Cl)nc(N)nc23)c1C
TargetHSP,Autophagy
Solubility10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.27 mM);DMSO:45 mg/mL (141.17 mM)

Bioactivity

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Target IC50
HSP90:1.7 nM(Ki)|HSP90:38 nM (EC50)
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.
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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.
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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)
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Storage & Handling

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StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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CNF 2024, CNF2024, CNF-2024, BIIB 021, BIIB021, BIIB-021, Autophagy, inhibit, HSP90, HSP, Heat shock proteins, Inhibitor

Similar Products

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  • BIIB021

    BIIB021 [orb1223865]

    >98% (HPLC)

    848695-25-0

    318.7615

    C14H15ClN6O

    1 g, 500 mg, 5 mg, 25 mg, 10 mg, 50 mg, 100 mg, 200 mg
Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at support@biorbyt.com.

Compound Identifiers

PubChem CID
16736529 ↗

Key Properties

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No computed properties available.

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BIIB021 (orb1305792)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

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5 mg
$ 80.00
1 ml x 10 mM (in DMSO)
$ 100.00
10 mg
$ 110.00
25 mg
$ 150.00
50 mg
$ 220.00
100 mg
$ 300.00
200 mg
$ 430.00
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