Geldanamycin

For research use only.

Catalog No.S2713 Synonyms: NSC 122750

13 publications

Geldanamycin Chemical Structure

Molecular Weight(MW): 560.64

Geldanamycin (NSC 122750) is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association. Geldanamycin attenuates virus infection-induced ALI (acute lung injury)/ARDS (acute respiratory distress syndrome) by reducing the host's inflammatory responses.

Size Price Stock Quantity  
10mM (1mL in DMSO) RMB 3131.63 In stock
RMB 1407.44 In stock
RMB 2229.39 In stock
RMB 5493.81 In stock
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Selleck's Geldanamycin has been cited by 13 publications

3 Customer Reviews

  • Phenotypic effect of Genetic or Pharmacologic Compromise of the 477 Hsp70-StiA-Hsp90 Complex. The impact of each genetic modification on radial growth, conidiation, and response to various stress conditions was assessed after inoculation of a suspension of 104 conidia on glucose minimal medium (GMM) agar plates and incubation at 37ºC for 5 days.

    Antimicrob Agents Chemother, 2015, 10.1128/AAC.00946-15. Geldanamycin purchased from Selleck.

  • C2C12 myoblasts were transfected with HA-tagged A17-PABPN1 constructs. Twenty-four hours post-transfection, cells were treated with CHX (10 μg/ml) alone or together with geldanamycin (2.5 μM) for the indicated times at 37°C. Lysates were blotted to show the expression of the proteins of interest. Band density was quantified and is shown in the line graph (right panels). Data are shown as the mean ± SEM (n = 5); **, P < 0.01.

    PLoS One, 2015, 10(9):e0138936.. Geldanamycin purchased from Selleck.

  • RT-qPCR analysis of eNOS mRNA and representative Western blot images of eNOS expression, respectively, in irradiated BAECs pretreated of geldanamycin (GA; 500 nM). At 12 h after 10 Gy irradiation, BAECs were harvested. The results suggest that both HSP90 is involved in the upregulation of eNOS in irradiated BAECs.

    Radiat Res, 2018, 189(5):519-528. Geldanamycin purchased from Selleck.

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Biological Activity

Description Geldanamycin (NSC 122750) is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association. Geldanamycin attenuates virus infection-induced ALI (acute lung injury)/ARDS (acute respiratory distress syndrome) by reducing the host's inflammatory responses.
Targets
p185 [4]
(SKBr3 cells)
HSP90 (N-terminal domain) [1]
(Cell-free assay)
HSP90 [1]
(Cell-free assay)
70 nM 0.78 μM(Kd) 1.2 μM(Kd)
In vitro

Geldanamycin binds in the ATP-binding site in the N-terminus domain of Hsp90s (residues 1-220). Geldanamycin inhibits the ATPase activity of Hsp90 in a dose-dependent manner. [1] Geldanamycin causes a dose-dependent G2 arrest and reversible inhibiton o f entry into the S phase in A2780 human ovarian cell line. This inhibition is accompanied by p53 increase and finally demonstrated to be p53 dependent. [2] Geldanamycin causes polyubiquitination and proteasomal degradation of the p185 receptor protein-tyrosin kinase and shows a IC50 with 70 nM. [3, 4] Geldanamycin is a typical anti-tumor reagent, shows a mean GI50 with 0.18 μM against the panel of 60 human tumor cell lines. [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A2780 cells MXLQdo9tcW[ncnH0bY9vKGG|c3H5 MljrR49ueG:3bnSge4F{KGW4YXz1ZZRm\CCob4KgZY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCxdnHybYFvKGOjcnPpco9u[SClZXzsJIxqdmViQUK3PFAtKEmFNUC9N{41KM7:TR?= NUDLZnJSOTF3MUSxOFU>
SW620 cell M3Hu[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkHxTY5pcWKrdH;yfUBkd26lZX70doF1cW:wIHHnZYlve3RiaIXtZY4h[2:ub4LlZ5RidCClYYLjbY5wdWFiU2e2NlAh[2WubDDsbY5meyxiSVO1NF03NjJibl2= M4npR|E2PjV6OEe5
MCF-7 cell M{HaT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUnJcohq[mm2b4L5JINwdmOnboTyZZRqd25iYXfhbY5{fCCqdX3hckBjemWjc4SgZ4Fv[2W{IF3DSk04KGOnbHygcIlv\XNuIFnDOVA:Pi53IH7N M2W5TFE2PjV6OEe5
SKBR3 cells NXP3O4hZWHKxbHnm[ZJifGmxbjDhd5NigQ>? NGXMco44OiCq MnfhRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDld5Rzd2enbjDy[YNmeHSxcjDk[YZq[2mnboSgbJVu[W5iU1vCVlMh[2WubIOgZYZ1\XJiN{KgbJJ{NCCLQ{WwQVgvPSCwTR?= MV6yN|Y1QDF6MB?=
MCF7 cells M2HzT3Bzd2yrZnXyZZRqd25iYYPzZZk> Mkj5O|IhcA>? M1S4NWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDlfJBz\XO|aX7nJIV{fHKxZ3XuJJJm[2WydH;yJIFnfGW{IEeyJIhzeyxiSVO1NF06Njhibl2= NHHFRXQzOzZ2OEG4NC=>
MDA-kb2 cells MoHjSpVv[3Srb36gZZN{[Xl? MmfCNVghcA>? NXr4ZlNkUW6qaXLpeIlwdiCxZjDIV3A6OCCrbjDoeY1idiCPRFGtb4IzKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDncJVkd2OxcoTpZ49q\CC{ZXPldJRwei2mZYDlcoRmdnRibIXjbYZmemG|ZTDlfJBz\XO|aX;uJIFnfGW{IEG4JIhzeyCkeTDmbZJm\my7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhUUN3ME2xNEBvVQ>? MknxNlQ6QDR7M{[=
human SK-BR-3 cells M3HFeHBzd2yrZnXyZZRqd25iYYPzZZk> NUXsbmlHSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT{1DWi1|IHPlcIx{NCCLQ{WwQVE2Njhibl2= MkHYNVk5QTZ6NEi=
HUVEC cells MoLkR5l1d3SxeHnjxsBie3OjeR?= NGXnd2Y4OiCq MXfDfZRwfG:6aXPpeJkh[WejaX7zeEBJXV[HQzDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVE6KG6P NYXMXpVpOjV{N{ewOlc>
human HCT116 cells NVvaR3RFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUnHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDIR3QyOTZiY3XscJMtKEeLNUC9NlEhdk1? NH2yepUyQDJ2M{ewNy=>
K562 cell NILnUpVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGPWV|JKdmirYnn0c5J6KGOxbnPlcpRz[XSrb36gZYdicW6|dDDoeY1idiCuZYXr[Y1q[SCNNU[yJINmdGxibHnu[ZMtKEmFNUC9NlIvOSCwTR?= NGPm[28yPTZ3OEi3PS=>
HT-29 cell MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MofsTY5pcWKrdH;yfUBkd26lZX70doF1cW:wIHHnZYlve3RiaIXtZY4h[2:ub4LlZ5RidCClYYLjbY5wdWFiSGStNlkh[2WubDDsbY5meyxiSVO1NF0zPC53IH7N NH[2U2IyPTZ3OEi3PS=>
HCT116 cells M{PkOXBzd2yrZnXyZZRqd25iYYPzZZk> NGPScnFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{BjgSCudX3pcoV{[2WwY3WgZZN{[XluIFXDOVA:OC5yMzFOwG0> M1nC[|IyPjB3OUe1
NCI-H1975 cells MWTQdo9tcW[ncnH0bY9vKGG|c3H5 MVjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3INVk4PSClZXzsd{whUUN3ME2zOkBvVQ>? NHO2RlczOTdzNUG2OS=>
human DLD1 cells NHjXem1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV3Hdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDEUGQyKGOnbHzzMEBIUTVyPUO3JI5O MX2xPFI1OzdyMx?=
human A431 cells Mk\ER5l1d3SxeHnjxsBie3OjeR?= NHTybms4OiCq M1zYS2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE1OzFiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME20NEBvVQ>? M2njcFI2Ojd5ME[3
human HepG2 cells MWTDfZRwfG:6aXRCpIF{e2G7 NV\FOHJ6PzJiaB?= M2DiWmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhmeEd{IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9OFAhdk1? MXSyOVI4PzB4Nx?=
human BGC823 cells NVXER215S3m2b4TvfIlkyqCjc4PhfS=> MYe3NkBp MoP6R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRmdEQDJ|IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9OFAhdk1? NG\Ee5EzPTJ5N{C2Oy=>
human SKBR3 cells NEe5bmFEgXSxdH;4bYPDqGG|c3H5 MVO3NkBp NHH5TmNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUU0KUMzDj[YxteyCjZoTldkA4OiCqcoOgZpkh[2WubITpeIVzNWeubzDhd5NigSxiSVO1NF01OSCwTR?= MoO4NVk1ODV3Mki=
human MDA-MB-231 cells MUXDfZRwfG:6aXRCpIF{e2G7 NF;kfng4OiCq NGf4dG1EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEFvTVKtNlMyKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;NUCgcm0> MmrlNlUzPzdyNke=
human A549 cells MXvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MULHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDBOVQ6KGOnbHzzMEBIUTVyPU[0JI5O MoLBNVgzPDN5MEO=
Sf9 cells NXjtW5pqTnWwY4Tpc44h[XO|YYm= MofMSIl{eGyjY3Xt[Y51KG:oIFfNMWJQTEmSWTDmdo9uKGi3bXHuJIZ2dGxibHXu[5RpKEiVUEmwJIFteGijIHX4dJJme3OnZDDpckBj[WO3bH;2bZJ2ey2rbn\lZ5Rm\CCVZkmgZ4VtdHNiYX\0[ZIhOTZiaILzJIJ6KG[udX;y[ZNk\W6lZTDwc4xiemm8YYTpc44h[XO|YYmsJGlEPTB;N{Sgcm0> NUnieotvOjR5NUG0OFE>
human U87MG cells MV3Qdo9tcW[ncnH0bY9vKGG|c3H5 MUPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFV6N13HJINmdGy|LDDJR|UxRTh7IH7N M3PhVlIyPzF3MU[1
human A549 cells MmDXR5l1d3SxeHnjxsBie3OjeR?= MlLaO|IhcA>? NWnJV3U{S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTV2OTDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVk4KG6P NWG4S4hJOjV{N{ewOlc>
mouse P19 cells MkXpR5l1d3SxeHnjxsBie3OjeR?= MoXmNVghcA>? MYLDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDQNVkh[2WubIOgZYZ1\XJiMUigbJJ{NCCLQ{WwQVAvOSEQvF2= NXLhXYFwOTd2NEK1OlU>
human HL7702 cells M3:zbGN6fG:2b4jpZ:Kh[XO|YYm= MYq3NkBp M33jO2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhNPzdyMjDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvOTRzIN88US=> Mlm5NlUzPzdyNke=
human A549 cells NUjYZW5ES3m2b4TvfIlkyqCjc4PhfS=> MlziNkBl[Xm| NID2c3BEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{KGGodHXyJFIh\GG7czDifUBCdGGvYYLCcJVmKGG|c3H5MEBKSzVyPUCuNVUh|ryP NYPvU2ZJOjN7NEe3PVQ>
human A431 cells Mmq4VJJwdGmoZYLheIlwdiCjc4PhfS=> MkPNO|IhcA>? NFvJcWRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG0N|Eh[2WubIOgZYZ1\XJiN{KgbJJ{NCCLQ{WwQVAvOiEQvF2= NUjSVmp5OjB4NUWyN|c>
human HepG2 cells NInWeHJEgXSxdH;4bYPDqGG|c3H5 NWDSVVNKS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWyR{KgZ4VtdHNiYomgUXRVKGG|c3H5MEBKSzVyPUCuN{DPxE1? M2TOcVI{PjV4NUW2
human SW480 cells MVPDfZRwfG:6aXRCpIF{e2G7 MYC3NkBp MmHDR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV3c1QDBiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlMyKM7:TR?= NEfEbJkzPTJ5N{C2Oy=>
human LNCAP cells NYfQVpZuS3m2b4TvfIlkyqCjc4PhfS=> M1;WeFczKGh? NEmyNnlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNVkODUDDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvPDNizszN NFi3bogzPTFyNUmyOC=>
human LS174T cells NWXBPZA{S3m2b4TvfIlkyqCjc4PhfS=> NE\veG9EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNWzF5NGSgZ4VtdHNiYomgUXRUKGG|c3H5MEBKSzVyPUCuOFUh|ryP M{LrXlE4ODN2MUO1
human HeLa cells NImwUmZEgXSxdH;4bYPDqGG|c3H5 NFr6epY4OiCq MnrRR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTIVN[SClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUCuO|k5KM7:TR?= NFXaOlczPTJ5N{C2Oy=>
rat L6 cells MVPDfZRwfG:6aXRCpIF{e2G7 Mln0O|IhcA>? MlrNR5l1d3SxeHnjbZR6KGGpYXnud5QhemG2IFy2JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCDbHHtZZIhSmy3ZTDhd5NigSxiSVO1NF02KM7:TR?= MWGyOFU5ODV|MR?=
human MCF7 cells MVHDfZRwfG:6aXRCpIF{e2G7 MojsR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{BjgSCVUlKgZZN{[XluIFnDOVA:QS54IN88US=> MYSxPVU3ODN3Mx?=
human MCF7 cells M3ftS2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NETOcVlIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBOS0Z5IHPlcIx{KGGodHXyJIRigXNiYomgV3JDKGG|c3H5MEBIUTVyPUO1MlYh|ryP NWrKXphCOTd6NkmwPVg>
HEK293T cells M1\pcGZ2dmO2aX;uJIF{e2G7 NYD6[YdNUW6qaXLpeIlwdiCxZjDUUmYu[WyyaHGtbY5lfWOnZDDOSk1s[XCyYVKgZYN1cX[jdHnvckBmgHC{ZYPz[YQhcW5iSFXLNlk{XCClZXzsd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYm= NETqc|kyQDRyOEexNy=>
human Jurkat cells MnjwSpVv[3Srb36gZZN{[Xl? MVHJcohq[mm2aX;uJI9nKFSQRj3hcJBp[S2rbnT1Z4VlKE6ILXvhdJBiSiCjY4TpeoF1cW:wIHX4dJJme3OnZDDpckBHSUSGIHTl[olkcWWwdDDoeY1idiCMdYLrZZQh[2WubIOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7 NILVUXgyQDRyOEexNy=>
human SKBR3 cells NU\6cXJCTnWwY4Tpc44h[XO|YYm= MXGyOEBp NVrXfVg5UW6qaXLpeIlwdiCxZjDId5A6OC2vZXTpZZRm\CCKRWKyJIRm\3KjZHH0bY9vKGmwIHj1cYFvKFONQmKzJINmdGy|IHHmeIVzKDJ2IHjyd{BjgSCZZYP0[ZJvKGKub4S= NY\F[JM2OTh6MU[xNVE>

... Click to View More Cell Line Experimental Data

In vivo Geldanamycin (50 mg//kg) shows 30% inhibition on pl85-associated phosphotyrosine levels in FRE/erbB-2 mice. [6]

Protocol

Kinase Assay:

[1]

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Isothermal Titration Calorimetry (ITC) of Nucelotide Binding:

The titration experiments are performed using the MSC system. In each experiment, 16 aliquots of 15 μL of geldanamycin (300 μM in 1% DMSO) are injected into 1.3 mL of protein (31 μM in 20 mMTris-HCl, pH 7.5, 1 mMEDTA) at 25 °C, and the resulting data are fit after subtracting the heats of dilution. Heats of dilution are determined in separate experiments from addition of geldanamycin into buffer and buffer into protein. No evidence for binding of DMSO in the nucleotide binding site is observed. Titration data are fit using a nonlinear least-squares curve-fitting algorithm with three floating variables: stoichiometry, binding constant (Kb) 1/Kd), and change of enthalpy of interaction (ΔH°). Dissociation constants estimated for geldanamycin binding to intact yeast Hsp90 is 1.22 μM, and for binding to Hsp90 N-terminal domain is 0.78 μM. No meaningful heat is observed with binding to the C-terminal fragment.
Cell Research:

[2]

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  • Cell lines: A2780 human ovarian cell line
  • Concentrations: 0.001-10 μM
  • Incubation Time: 3 hours
  • Method:

    Exponentially growing cells are treated with Geldanamycin and at various times DNA synthesis is assessed by incorporation of bromodeoxyuridine (BrdUrd) and flow cytometric analysis. No marked difference in total cell number is noted during this time course for treated and untreated cultures. BrdUrd (10 μM) is incorporated over a 4-h incubation period at 37 °C and cells are harvested and fixed in 70% ethanol. After denaturation of the DNA with 2 N HC1, cells are incubated with an anti-BrdUrd mouse monoclonal antibody followed by a fluorescein isothiocyanate (FITC)-linked goat anti-mouse IgG. Cells are stained for 30 minutes at room temperature with propidium iodide and analysed by flow cytometry using a Coulter EPICS Profile Analyzer.


    (Only for Reference)
Animal Research:

[6]

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  • Animal Models: FRE/erbB-2 tumors in nu/nu mice
  • Dosages: 50 mg/kg
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 36 mg/mL warmed (64.21 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 560.64
Formula

C29H40N2O9

CAS No. 30562-34-6
Storage powder
in solvent
Synonyms NSC 122750
Smiles CC1CC(C(C(C=C(C(C(C=CC=C(C(=O)NC2=CC(=O)C(=C(C1)C2=O)OC)C)OC)OC(=O)N)C)C)O)OC

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00003969 Completed Drug: tanespimycin Unspecified Adult Solid Tumor Protocol Specific Cancer Research UK|National Cancer Institute (NCI) August 1998 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID