.product-side h2 span {width: 50%;}.product-side h2 span.hover {}Related ProductsAUY922 (NVP-AUY922)PF-04929113 (SNX-5422)IPI-504 (Retaspimycin hydrochloride)XL-888MPC-3100AT13387Molarity CalculatorDilution Calculator BIIB021Hsp90 inhibitor,selective and competitiveCatalog No.A4058SizePriceStockQty10mM (in 1mL DMSO)$61.00In stock 5mg$55.00In stock 10mg$80.00In stock 50mg$210.00In stock 100mg$320.00In stock Tel: +1-832-696-8203Email: sales@apexbt.comWorldwide Distributors Add to CartBulk InquiryFree samples Check OutSample solution is provided at 25 µL, 10mM.Publications citing ApexBio ProductsNature.2017 Jan 19;541(7637):417-420.Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Related Compound Libraries DiscoveryProbe™ Bioactive Compound LibraryDiscoveryProbe™ Anti-cancer Compound LibraryDiscoveryProbe™ Metabolism-related Compound LibraryDiscoveryProbe™ Protease Inhibitor LibraryQuality Control Quality Control & MSDS View current batch: 1 Purity = 99.51% COA (Certificate Of Analysis) HPLC (Retest) NMR (Nuclear Magnetic Resonance) MSDS (Material Safety Data Sheet) Datasheet Chemical structure Biological ActivityDescriptionBIIB021 is a selective and competitive inhibitor of Hsp90 with Ki value of 1.7 nM.TargetsHsp90IC501.7 nM (Ki)BIIB021 Dilution CalculatorConcentration (start)xVolume (start)=Concentration (final)xVolume (final) femtomolar picomolar nanomolar micromolar millimolar molar nanoliter microliter milliliter liter femtomolar picomolar nanomolar micromolar millimolar molar microliter milliliter liter C1V1C2V2calculateBIIB021 Molarity CalculatorMass=ConcentrationxVolumexMW* picograms nanograms micrograms milligrams grams kilograms femtomolar picomolar nanomolar micromolar millimolar molar nanoliter microliter milliliter liter g/molcalculate Chemical Properties Cas No. 848695-25-0SDF Download SDF Synonyms N/A Chemical Name 6-chloro-9-[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]purin-2-amine Canonical SMILES CC1=CN=C(C(=C1OC)C)CN2C=NC3=C2N=C(N=C3Cl)N Formula C14H15ClN6O M.Wt 318.8 Solubility ≥14.95 mg/mL in DMSO, Storage Store at -20°CPhysical AppearanceA solidShipping ConditionEvaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon requestGeneral tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. BackgroundBIIB021 is a selective inhibitor of Hsp90 with Ki and EC50 values of 1.7 nM and 38 nM, respectively.[1] HSP90 (heat shock protein 90) is widely expressed as a molecular chaperone. It plays a major role in the folding and stabilization of cellular proteins. HSP90 protects client proteins from degradation and maintains them in an active conformation. Many clients of HSP90 are transcription factors or protein kinases such as: Bcr-Abl, tyrosine kinases, EGFR family members, IGF1-R, c-Met, steroid hormone receptors, p53, Mdm2 and telomerase. In a variety of cancers, overexpressed hsp90 has been found. Hsp90 also play an important role in maintaining the transformed phenotype of cancer cells so. Hsp 90 is one attractive target for cancer therapy.[2]BIIB021 competitive binds in the ATP-binding pocket and inhibits Hsp90 chaperone function, and lead to client protein degradation, cell death and tumor growth inhibition. BIIB021 leads to degradation of HER-2 which is an Hsp90 client protein. BIIB021 can also the growth of a variety of cancer cell lines in cell proliferation assays. In MCF-7 cells, BIIB021 leaded to HER-2 degradation with the EC50 value of was38 ± 10 nmol/L. BIIB021 inhibit the cell proliferation with IC50 values of 0.06 μ mol/L in N87 cells, 0.31μ mol/L in MCF-7 cells and 0.14 μ mol/L in BT474 cells. In MCF-7 cells, BIIB021 significantly reduced the phosphorylation levels of HER-2 at a concentration of 50 nM.[1] BIIB021 selectively inhibited Hodgkin"s lymphoma cell viability at nanomolar concentrations but not in lymphocytes from healthy individuals. BIIB021 can increase the susceptibility to NK cell mediated killing by inducing the expression of ligands for the activating NK cell receptor NKG2D on Hodgkin"s lymphoma cells.[3] BIIB021 reduced the expression of key radioresponsive proteins, then enhanced the radiosensitivity of HNSCCA cell lines in vitro, increased apoptosis cells and induced G2 arrest.[2]BIIB021 showed significant activity at doses of 31,62.5, and 125 mg/kg in human in nude mice bearing N87 stomach carcinoma tumors.[1] HSP90 significantly inhibited tumor growth in a xenograft model of Hodgkin"s lymphoma.[1]References: 1.Lundgren K, Zhang H, Brekken J, Huser N, Powell RE, Timple N, Busch DJ, Neely L, Sensintaffar JL, Yang YC et al: BIIB021, an orally available, fully synthetic small-molecule inhibitor of the heat shock protein Hsp90. Mol Cancer Ther 2009, 8(4):921-929.2.Yin X, Zhang H, Lundgren K, Wilson L, Burrows F, Shores CG: BIIB021, a novel Hsp90 inhibitor, sensitizes head and neck squamous cell carcinoma to radiotherapy. Int J Cancer 2010, 126(5):1216-1225.3.Boll B, Eltaib F, Reiners KS, von Tresckow B, Tawadros S, Simhadri VR, Burrows FJ, Lundgren K, Hansen HP, Engert A 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, 15(16):5108-5116.