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Chemical Structure| 30562-34-6 Chemical Structure| 30562-34-6

Structure of Geldanamycin
CAS No.: 30562-34-6

Chemical Structure| 30562-34-6

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Geldanamycin is an Hsp90 inhibitor with antimicrobial activity against many Gram-positive and some Gram-negative bacteria and also exhibits anti-influenza virus H5N1 activities.

Synonyms: NSC 122750

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Product Details of Geldanamycin

CAS No. :30562-34-6
Formula : C29H40N2O9
M.W : 560.64
SMILES Code : NC(O[C@H](/C(C)=C/[C@@H](C)[C@H](O)[C@H](OC)C[C@H](C)CC1=C2OC)[C@H](OC)/C=C/C=C(C)/C(NC(C1=O)=CC2=O)=O)=O
Synonyms :
NSC 122750
MDL No. :MFCD00274570

Safety of Geldanamycin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H332-H335
Precautionary Statements:P261-P280-P305+P351+P338

Related Pathways of Geldanamycin

DNA

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
human monocyte-derived dendritic cells (MO-DCs) 0.1 μM 48 hours To assess the effects of GA on the iμMuno-phenotype and functions of MO-DCs. GA partially activated unstimulated MO-DCs but interfered with their full maturation during stimulation, accompanied by impaired upregulation of RelB. PMC3926270
HEK293T cells 0.1 μM 24 hours To assess the effects of GA on transcription factor activities. GA had no effect on AP1 and NFAT under basal conditions but slightly inhibited CREB and STAT1/2, while moderately enhancing NF-κB activity. PMC3926270
HCT116 p53+/+ cells 1 μM 15 hours later GA treatment had no significant effect on G2 arrest in p53 wild-type cells, maintaining the G2 arrest. PMC2811229
HCT116 p53-/- cells 1 μM 15 hours later GA treatment significantly reduced G2/M arrest in p53-deficient cells, pushing cells into premature mitosis. PMC2811229
HT-29 cells 1 μM 15 hours later GA treatment enhanced the mitotic cell population in HT-29 cells, pushing cells into premature mitosis. PMC2811229
Primary human airway epithelia 25 μM 21 days Geldanamycin prevented IL-13-induced goblet cell metaplasia and reduced the proportion of PAS-positive cells. PMC6355221
Primary human airway epithelia 25 μM 14 days Geldanamycin reverted IL-13-induced goblet cell metaplasia and reduced the number of goblet cells. PMC6355221

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
mice carrageenan-induced paw edema model intraperitoneal injection 35 mg/kg once daily, throughout the experimental period Geldanamycin significantly inhibited carrageenan-induced paw edema in a dose-dependent manner PMC1572305
Mice IL-13-induced goblet cell metaplasia model Intranasal delivery 25 mg/kg Once daily for 5 days Geldanamycin prevented IL-13-induced airway goblet cell metaplasia and reduced the abundance of goblet cells. PMC6355221

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01193491 Hematologic Malignancies Phase 1 Terminated(Drug exposure of re... More >>taspimycin HCl was superior to IPI-493, Infinity will focus on Retaspimycin HCL) Less << - United States, Maryland ... More >> Johns Hopkins Sidney Kimmel Cancer Center Baltimore, Maryland, United States, 21201 United States, New York Weill Cornell Cancer Center New York, New York, United States, 10065 United States, Texas M.D. Anderson Cancer Center Houston, Texas, United States, 77030 Less <<
NCT00319930 Chronic Lymphocytic Leukemia Phase 1 Terminated(Discontinuation of ... More >>program) Less << - United States, Florida ... More >> Ocoee, Florida, United States, 34761 United States, New York Albany, New York, United States, 12208 United States, Ohio Dayton, Ohio, United States, 45409 United States, South Carolina Greenville, South Carolina, United States, 29605 United States, Texas Tyler, Texas, United States, 75702 United States, Virginia Norfolk, Virginia, United States, 85258 Less <<
NCT00093821 Childhood Chronic Myelogenous ... More >>Leukemia Childhood Desmoplastic Small Round Cell Tumor Disseminated Neuroblastoma Metastatic Childhood Soft Tissue Sarcoma Metastatic Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor Metastatic Osteosarcoma Previously Treated Childhood Rhabdomyosarcoma Recurrent Childhood Acute Lymphoblastic Leukemia Recurrent Childhood Acute Myeloid Leukemia Recurrent Childhood Rhabdomyosarcoma Recurrent Childhood Soft Tissue Sarcoma Recurrent Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor Recurrent Neuroblastoma Recurrent Osteosarcoma Less << Phase 1 Completed - United States, New York ... More >> Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10065 Less <<
NCT00119236 Unspecified Adult Solid Tumor,... More >> Protocol Specific Less << Phase 1 Completed - United States, New York ... More >> Memorial Sloan Kettering Cancer Center New York, New York, United States, 10065 Less <<
NCT00087386 Recurrent Melanoma ... More >> Stage III Melanoma Stage IV Melanoma Less << Phase 2 Terminated - United States, New York ... More >> Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10065 Less <<
NCT00058253 Recurrent Prostate Cancer ... More >> Stage IV Prostate Cancer Unspecified Adult Solid Tumor, Protocol Specific Less << Phase 1 Completed - United States, New York ... More >> Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10065 Less <<
NCT00004065 Bladder Cancer ... More >> Breast Cancer Colorectal Cancer Gastric Cancer Head and Neck Cancer Kidney Cancer Leukemia Lung Cancer Melanoma (Skin) Ovarian Cancer Prostate Cancer Unspecified Adult Solid Tumor, Protocol Specific Less << Phase 1 Completed - United States, California ... More >> Jonsson Comprehensive Cancer Center, UCLA Los Angeles, California, United States, 90095 United States, New York Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10021 Less <<
NCT00093405 Kidney Cancer Phase 2 Completed - United States, New York ... More >> Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10021 Less <<
NCT00003969 Unspecified Adult Solid Tumor,... More >> Protocol Specific Less << Phase 1 Completed - United Kingdom ... More >> Royal Marsden NHS Foundation Trust - London London, England, United Kingdom, SW3 6JJ Less <<
NCT00019708 Extranodal Marginal Zone B-cel... More >>l Lymphoma of Mucosa-associated Lymphoid Tissue Nodal Marginal Zone B-cell Lymphoma Non-Hodgkin 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 Immunoblastic Large Cell Lymphoma Recurrent Adult Lymphoblastic Lymphoma Recurrent Grade 1 Follicular Lymphoma Recurrent Grade 2 Follicular Lymphoma Recurrent Grade 3 Follicular Lymphoma Recurrent Marginal Zone Lymphoma Recurrent Small Lymphocytic Lymphoma Splenic Marginal Zone Lymphoma Stage IV Adult Burkitt Lymphoma Stage IV Adult Diffuse Large Cell Lymphoma Stage IV Adult Diffuse Mixed Cell Lymphoma Stage IV Adult Diffuse Small Cleaved Cell Lymphoma Stage IV Adult Immunoblastic Large Cell Lymphoma Stage IV Adult Lymphoblastic Lymphoma Stage IV Grade 1 Follicular Lymphoma Stage IV Grade 2 Follicular Lymphoma Stage IV Grade 3 Follicular Lymphoma Stage IV Mantle Cell Lymphoma Stage IV Marginal Zone Lymphoma Stage IV Small Lymphocytic Lymphoma Unspecified Adult Solid Tumor, Protocol Specific Less << Phase 1 Terminated - United States, Nebraska ... More >> University of Nebraska Medical Center Omaha, Nebraska, United States, 68198 Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.78mL

0.36mL

0.18mL

8.92mL

1.78mL

0.89mL

17.84mL

3.57mL

1.78mL

References

 

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