1. Cell Cycle/DNA Damage
    Metabolic Enzyme/Protease
  2. HSP

Alvespimycin (Synonyms: 17-DMAG; KOS-1022; NSC 707545)

Cat. No.: HY-10389
Handling Instructions

Alvespimycin (17-DMAG; KOS-1022; NSC 707545) is a potent, water-soluble HSP90 inhibitor with IC50 of 62 nM.

For research use only. We do not sell to patients.
Alvespimycin Chemical Structure

Alvespimycin Chemical Structure

CAS No. : 467214-20-6

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Customer Review

Other Forms of Alvespimycin:

    Alvespimycin purchased from MCE. Usage Cited in: Friedrich-Alexander University Erlangen-Nuremberg. 2016.

    pJAK2 and JAK2 expression upon TGFβ stimulation and JAK inhibitors incubation. pJAK2 and JAK2 expression in healthy human fibroblasts after stimulation with TGFβ for 3 days and incubation with TG101209, 17-DMAG or Ruxolitinib.
    • Biological Activity

    • Protocol

    • Technical Information

    • References

    Description

    Alvespimycin (17-DMAG; KOS-1022; NSC 707545) is a potent, water-soluble HSP90 inhibitor with IC50 of 62 nM. IC50 Value: 62 nM Target: HSP90 in vitro: 17-DMAG displays ~2 times potency against human Hsp90 than 17-AAG, with IC50 of 62 nM versus 119 nM. In SKBR3 and SKOV3 cells which over-express Hsp90 client protein Her2, 17-DMAG causes down-regulation of Her2 with EC50 of 8 nM and 46 nM, respectively, as well as induction of Hsp70 with EC50 of 4 nM and 14 nM, respectively, leading to significant cytotoxicity with GI50 of 29 nM and 32 nM, respectively, consistent with Hsp90 inhibition. 17-DMAG in combination with vorinostat synergistically induces apoptosis of the cultured MCL cells as well as primary MCL cells, more potently than either agent alone, by markedly attenuating the levels of cyclin D1 and CDK4, as well as of c-Myc, c-RAF and Akt. in vivo: 17-DMAG treatment at 5 mg/kg or 25 mg/kg thrice per week significantly reduces tumor growth of TMK-1 xenografts, by significantly reducing vessel area and numbers of proliferating tumor cells in sections. Consistent the inhibition of FAK signaling in vivo, 17-DMAG treatment at 25 mg/kg three times a week significantly suppresses tumor growth, and metastasis of ME180 and SiHa xenografts in mice. Administration of 17-DMAG at 10 mg/kg for 16 days significantly decreases the white blood cell count and prolongs the survival in a TCL1-SCID transplant mouse model.

    Clinical Trial
    NCT Number Sponsor Condition Start Date Phase
    NCT00089271 National Cancer Institute (NCI) Anaplastic Large Cell Lymphoma|Angioimmunoblastic T-cell Lymphoma|Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Intraocular Lymphoma|Nodal Marginal Zone B-cell Lymphoma|Recurrent Adult Burkitt Lymphoma|Recurrent Adult Diffuse Large Cell Lymphoma|Recurrent Adult Diffuse Mixed Cell Lymphoma|Recurrent Adult Diffuse Small Cleaved Cell Lymphoma|Recurrent Adult Hodgkin Lymphoma|Recurrent Adult T-cell Leukemia/Lymphoma|Recurrent Cutaneous T-cell Non-Hodgkin Lymphoma|Recu July 2004 Phase 1
    NCT00089362 National Cancer Institute (NCI) Male Breast Cancer|Recurrent Adenoid Cystic Carcinoma of the Oral Cavity|Recurrent Basal Cell Carcinoma of the Lip|Recurrent Breast Cancer|Recurrent Colon Cancer|Recurrent Esthesioneuroblastoma of the Paranasal Sinus and Nasal Cavity|Recurrent Gastric Cancer|Recurrent Inverted Papilloma of the Paranasal Sinus and Nasal Cavity|Recurrent Lymphoepithelioma of the Nasopharynx|Recurrent Lymphoepithelioma of the Oropharynx|Recurrent Melanoma|Recurrent Metastatic Squamous Neck Cancer With Occult Primar July 2004 Phase 1
    NCT00780000 Bristol-Myers Squibb Breast Cancer April 2008 Phase 2
    NCT01126502 National Cancer Institute (NCI) B-cell Chronic Lymphocytic Leukemia|Prolymphocytic Leukemia|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia May 2010 Phase 1
    NCT00248521 Institute of Cancer Research, United Kingdom|National Cancer Institute (NCI) Unspecified Adult Solid Tumor, Protocol Specific October 2005 Phase 1
    NCT00803556 Bristol-Myers Squibb Solid Tumor|Breast Cancer January 2006 Phase 1
    NCT00088868 National Institutes of Health Clinical Center (CC)|National Cancer Institute (NCI) Lymphoma|Small Intestine Cancer|Unspecified Adult Solid Tumor, Protocol Specific June 2004 Phase 1
    NCT00089271 National Cancer Institute (NCI) Anaplastic Large Cell Lymphoma|Angioimmunoblastic T-cell Lymphoma|Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Intraocular Lymphoma|Nodal Marginal Zone B-cell Lymphoma|Recurrent Adult Burkitt Lymphoma|Recurrent Adult Diffuse Large Cell Lymphoma|Recurrent Adult Diffuse Mixed Cell Lymphoma|Recurrent Adult Diffuse Small Cleaved Cell Lymphoma|Recurrent Adult Hodgkin Lymphoma|Recurrent Adult T-cell Leukemia/Lymphoma|Recurrent Cutaneous T-cell Non-Hodgkin Lymphoma|Recu July 2004 Phase 1
    NCT00089362 National Cancer Institute (NCI) Male Breast Cancer|Recurrent Adenoid Cystic Carcinoma of the Oral Cavity|Recurrent Basal Cell Carcinoma of the Lip|Recurrent Breast Cancer|Recurrent Colon Cancer|Recurrent Esthesioneuroblastoma of the Paranasal Sinus and Nasal Cavity|Recurrent Gastric Cancer|Recurrent Inverted Papilloma of the Paranasal Sinus and Nasal Cavity|Recurrent Lymphoepithelioma of the Nasopharynx|Recurrent Lymphoepithelioma of the Oropharynx|Recurrent Melanoma|Recurrent Metastatic Squamous Neck Cancer With Occult Primar July 2004 Phase 1
    NCT00780000 Bristol-Myers Squibb Breast Cancer April 2008 Phase 2
    NCT01126502 National Cancer Institute (NCI) B-cell Chronic Lymphocytic Leukemia|Prolymphocytic Leukemia|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia May 2010 Phase 1
    NCT00248521 Institute of Cancer Research, United Kingdom|National Cancer Institute (NCI) Unspecified Adult Solid Tumor, Protocol Specific October 2005 Phase 1
    NCT00803556 Bristol-Myers Squibb Solid Tumor|Breast Cancer January 2006 Phase 1
    NCT00088868 National Institutes of Health Clinical Center (CC)|National Cancer Institute (NCI) Lymphoma|Small Intestine Cancer|Unspecified Adult Solid Tumor, Protocol Specific June 2004 Phase 1
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    References
    Molecular Weight

    616.75

    Formula

    C₃₂H₄₈N₄O₈

    CAS No.

    467214-20-6

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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    Product Name:
    Alvespimycin
    Cat. No.:
    HY-10389
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