Name: Alvespimycin (17-DMAG) HCl
Brand: Selleck Chemicals
SKU: S1142
Rating: 5 (54 reviews)

Alvespimycin (17-DMAG) HCl Chemical Structure

CAS No. 467214-21-7

Selleck's Alvespimycin (17-DMAG) HCl has been cited by 54 publications

Purity & Quality Control

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HSP (HSP90) Signaling Pathway Map

Biological Activity

Description

Alvespimycin (17-DMAG, NSC 707545, BMS 826476, KOS 1022) HCl is a potent HSP90 inhibitor with IC50 of 62 nM in a cell-free assay. Phase 2.

Features

A synthetic derivative Geldanamycin, with lower hepatotoxicity than parent antibiotic & higher potency and bioavailability than the similar derivative 17-AAG.

Targets

HSP90 ^[1]
(Cell-free assay)

62 nM

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. ^[1] 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. ^[3] In contrast to 17-AAG which is only active for IKKβ in chronic lymphocytic leukemia (CLL) cells, 17-DMAG treatment effectively leads to depletion of the Hsp90 client protein, resulting in diminished NF-κB p50/p65 DNA binding, decreased NF-κB target gene transcription, and caspase-dependent apoptosis. By targeting the NF-κB family, 17-DMAG selectively mediates dose- and time-dependent cytotoxicity against CLL cells, but not normal T cells or NK cells important for immune surveillance. ^[5]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID

SKBr3	M2r0S2N6fG:2b4jpZ4l1gSCjc4PhfS=>			NETlUnJEgXSxdH;4bYNqfHliYXfhbY5{fCCVS1LyN{Bk\WyuczygTWM2OD1yLkCyOO69VS5?	NFm0OZk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNkG2OVM2PCd-MU[xOlU{PTR:L3G+
SKBR3	MnHpSpVv[3Srb36gZZN{[Xl?			NGfmXGpWeHKnZ4XsZZRqd25ib3[gTJNxPzBiaX6gV2tDWjNiY3XscJMtKEWFNUC9NE4xODUQvF2u	MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjh3NEC2Okc,OTZ6NUSwOlY9N2F-
SKBR3	MWHGeY5kfGmxbjDhd5NigQ>?			M3jHWmRm\3KjZHH0bY9vKG:oIFjldlIhcW5iU1vCVlMh[2WubIOsJGVEPTB;MD6wNFjPxE1w	MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjh3NEC2Okc,OTZ6NUSwOlY9N2F-
SKOV3	M1[xbmZ2dmO2aX;uJIF{e2G7			NVPpOoFQXXC{ZXf1cIF1cW:wIH;mJGh{eDdyIHnuJHNMV1Z\|IHPlcIx{NCCHQ{WwQVAvODF2zszNMi=>	MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjh3NEC2Okc,OTZ6NUSwOlY9N2F-
SKOV3	MWDGeY5kfGmxbjDhd5NigQ>?			NFnKc25F\We{YXTheIlwdiCxZjDI[ZIzKGmwIGPLU3Y{KGOnbHzzMEBGSzVyPUCuNFQ3\|ryPLh?=	MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjh3NEC2Okc,OTZ6NUSwOlY9N2F-
AGS	M2P1VmZ2dmO2aX;uJIF{e2G7		Ml;VNVYhcHK\|	NIfjUYlKdmirYnn0bY9vKG:oIFjJSlEh[WO2aY\heIlwdiCrbjDoeY1idiCDR2OgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCqeYDvfIliNWmwZIXj[YQhdHWlaX\ldoF{\SCneIDy[ZN{cW:wIHHmeIVzKDF4IHjyd{BjgSC{ZYDvdpRmeiCjc4PhfUwhUUN3ME2wMlA{Ps7:TT6=	MlvJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd3OEO5OVAoRjF5NUizPVUxRC:jPh?=
Hep3B	M135[mZ2dmO2aX;uJIF{e2G7		NV;sV\|RmOTZiaILz	Moj3TY5pcWKrdHnvckBw\iCKSV[xJIFkfGm4YYTpc44hcW5iaIXtZY4hUGWyM1KgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCqeYDvfIliNWmwZIXj[YQhdHWlaX\ldoF{\SCneIDy[ZN{cW:wIHHmeIVzKDF4IHjyd{BjgSC{ZYDvdpRmeiCjc4PhfUwhUUN3ME2wMlA3Oc7:TT6=	NELUOXc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{W4N\|k2OCd-MUe1PFM6PTB:L3G+
AGS	MVTGeY5kfGmxbjDhd5NigQ>?		M1LEeFI1KGi{cx?=	Mn:xWoli[mmuaYT5JI9nKGi3bXHuJGFIWyClZXzsd{B2dmSncjDuc5Jud3irYzDjc45lcXSrb37zJIFnfGW{IEK0JIhzeyCkeTDNWHQh[XO\|YYmsJGlEPTB;MUdOwG0v	MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV6M{m1NEc,OTd3OEO5OVA9N2F-
NCI-H526	NIG0e29HfW6ldHnvckBie3OjeR?=	NHS0VZMyKHWP	NIe1RZIzPCCqcoO=	NH\sNFFDcW6maX7nJIFn\mmwaYT5JJRwKEiVUEmwJIlvKGi3bXHuJG5EUS2KNUK2JINmdGy\|IHH0JFEhfU1iYX\0[ZIhOjRiaILzJIJ6KG[udX;y[ZNk\W6lZTDwc4xiemm8YYTpc44h[XO\|YYm=	NHnYZ\|c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{[wN\|U1OCd-MUe2NFM2PDB:L3G+
NCI-H526	MXTGeY5kfGmxbjDhd5NigQ>?	MlH2NUB2VQ>?	NXPLbHRIQTZiaILz	Mke0TY5pcWKrdHnvckBw\iCKU2C5NE1u\WSrYYTl[EBxem:uaX\ldoF1cW:wIH;mJIh2dWGwIF7DTU1JPTJ4IHPlcIx{KGG2IEGgeW0h[W[2ZYKgPVYhcHK\|IHL5JJN2dG[xcnjv[IFucW6nIFKgZZN{[Xl?	NH;leIw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{[wN\|U1OCd-MUe2NFM2PDB:L3G+
AGS	NHnkPGNHfW6ldHnvckBie3OjeR?=			NHT4bVBKdmirYnn0bY9vKG:oIHj5dI95cWFvaX7keYNm\CCKSV[xJIFkfGm4YYTpc44hcW5iaIXtZY4hSUeVIHPlcIx{KGK7IILldI9zfGW{IHflcoUh[XO\|YYmsJGlEPTB;MD6wNFM3\|ryPLh?=	M3;lXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6M{W5OlMyLz5zOEO1PVY{OTxxYU6=
HeLa	MYDGeY5kfGmxbjDhd5NigQ>?			MY\Jcohq[mm2aX;uJI9nKFSQRj3hcJBp[S2rbnT1Z4VlKE6ILXvhdJBiSiCjY4TpeoF1cW:wIHnuJIh2dWGwIFjlUIEh[2WubIOsJGlEPTB;MD6xOe69VS5?	NYqwXJZJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUizOVk3OzFpPkG4N\|U6PjNzPD;hQi=>
HeLa	M3TET2N6fG:2b4jpZ4l1gSCjc4PhfS=>			NYrK[2xbS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWOYTDj[YxteyCkeTDNWHQh[XO\|YYmsJGlEPTB;Mj6wOu69VS5?	NEDsUoE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEO1PVY{OSd-MUizOVk3OzF:L3G+
AGS	NWTL[XVpS3m2b4TvfIlkcXS7IHHzd4F6			NIPU[Y5EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCT1NiY3XscJMh[nliTWTUJIF{e2G7LDDJR\|UxRTF4zszNMi=>	NFjIS\|U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEO1PVY{OSd-MUizOVk3OzF:L3G+
A2058	M1\UcGN6fG:2b4jpZ4l1gSCjc4PhfS=>			NYK4ZndDS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTJyNUigZ4VtdHNiYomgUXRVKGG\|c3H5MEBKSzVyPUCuNFAzOc7:TT6=	MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDl{OUS4Okc,OTh7Mkm0PFY9N2F-
MDA-MB-231	NVqy[XJiTnWwY4Tpc44h[XO\|YYm=			MYLJcohq[mm2aX;uJI9nKEi\|cEmwJIlvKGi3bXHuJG1FSS2PQj2yN\|Eh[2WubIOgZZN{\XO\|ZXSgZZMhcGW{MjDk[Ydz[WSjdHnvckwhUUN3ME2wMlAxPDYQvF2u	M3yyN\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6OUK5OFg3Lz5zOEmyPVQ5PjxxYU6=
MDA-MB-231	NUTRV2t5S3m2b4TvfIlkcXS7IHHzd4F6			MX\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy\|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlAxPTkQvF2u	MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDl{OUS4Okc,OTh7Mkm0PFY9N2F-
A2058	NEe3V3NHfW6ldHnvckBie3OjeR?=			Mn\XTY5pcWKrdHnvckBw\iCKc4C5NEBqdiCqdX3hckBCOjB3ODDj[YxteyxiRVO1NF0xNjByN{pOwG0v	Mn3xQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh7Mkm0PFYoRjF6OUK5OFg3RC:jPh?=
MDA-MB-231	NEDtcnFHfW6ldHnvckBie3OjeR?=			MkTDTY5pcWKrdHnvckBw\iCKc4C5NEBqdiCqdX3hckBOTEFvTVKtNlMyKGOnbHzzJIF{e2W\|c3XkJIF{KEGtdDDk[Ydz[WSjdHnvckwhUUN3ME2wMlAyPzcQvF2u	M3rPOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6OUK5OFg3Lz5zOEmyPVQ5PjxxYU6=
A2058	NX3oVZhuTnWwY4Tpc44h[XO\|YYm=			NG\PVmpKdmirYnn0bY9vKG:oIFjzdFkxKGmwIHj1cYFvKEF{MEW4JINmdGy\|IHHzd4V{e2WmIHHzJGFsfCCmZXfyZYRifGmxbjygTWM2OD1yLkCyOFPPxE1w	MlHaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh7Mkm0PFYoRjF6OUK5OFg3RC:jPh?=
HuH7	MnHQRY51cX[rcnHsJIF{e2G7		NGLWWGE{KGSjeYO=	MULBcpRqfmm{YXygZYN1cX[rdImgZYdicW6\|dDDI[ZBifGm2aYOgR{B3cXK3czDn[Y5wfHmyZTCxZkBEd25zIHnu[oVkfGWmIHnuJIh2dWGwIFj1TFch[2WubIOgZZN{\XO\|ZXSgZZMhT0GSRFigVm5CKG:{IEG4V{BzWk6DIHzleoVtKGGodHXyJFMh\GG7czDifUByWlRvUFPSJIFv[Wy7c3nzMEBGSzVyPUCuNFAyOs7:TT6=	MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDl\|NkG5NUc,OTh7M{[xPVE9N2F-
HuH7	NYLNNmNbSW62aY\pdoFtKGG\|c3H5		MoHUN{Bl[Xm\|	Mn\kRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTIVx[XSrdHnzJGMhfmm{dYOg[4Vvd3S7cHWgNYIhS2:wMTDpcoZm[3SnZDDpckBpfW2jbjDIeWg4KGOnbHzzJIF{e2W\|c3XkJIF{KEeDUFTIJHJPSSCxcjCxPHMhelKQQTDs[ZZmdCCjZoTldkA{KGSjeYOgd4Vt\WO2ZXSge4l1cCB2MDDuUUBJS1ZvN{m2JIFv\CB6MECgcm0h[m:lZYDy[ZZqeiCkeTDxVnQuWEOUIHHuZYx6e2m\|LDDFR\|UxRTBwMECzNe69VS5?	NYS4PZEyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi5N\|YyQTFpPkG4PVM3OTlzPD;hQi=>
SKBR3	Mk[2SpVv[3Srb36gZZN{[Xl?			MVrCbY5lcW6pIHHm[olvcXS7IITvJGh{eDlyIHnuJIh2dWGwIGPLRnI{KGOnbHzzMEBKSzVyPUCuNFI1\|ryPLh?=	NYPlTpAzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmwNVc2PjJpPkG5NFE4PTZ{PD;hQi=>
Hep3B	MWrGeY5kfGmxbjDhd5NigQ>?		M1jHT\|MxKG2rboO=	MYPJcohq[mm2aX;uJI9nKGi7cH;4bYEucW6mdXPl[EBJUUZzYXzwbIEheHKxdHXpckBi[2O3bYXsZZRqd25iaX6gbJVu[W5iSHXwN2Ih[2WubIOgeJJm[XSnZDDmc5IhOzBibXnud{Bu\WG\|dYLl[EBi\nSncjCxNkBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{NCCLQ{WwQVAvODV5Mt88UU4>	M{fzNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MEeyNlE1Lz5zOUC3NlIyPDxxYU6=
Hep3B	NVH3WXE3TnWwY4Tpc44h[XO\|YYm=		MoLzNVYhcHK\|	NVi4dWVlUW6qaXLpeIlwdiCxZjDofZBwgGmjLXnu[JVk\WRiVlXHSkBxem:2ZXnuJJNm[3KndHnvckBqdiCqdX3hckBJ\XB\|QjDj[YxteyCjZoTldkAyPiCqcoOgZpkhTUyLU1GsJGlEPTB;MD6wO\|k2\|ryPLh?=	NGjoOGY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUC3NlIyPCd-MUmwO\|IzOTR:L3G+
HCT116	NXXldm9wS3m2b4TvfIlkcXS7IHHzd4F6		MmHWO\|IhcHK\|	Mln0R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGGodHXyJFczKGi{czygTWM2OD1yLkC1O:69VS5?	MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTJ\|MUi2OEc,OTl{M{G4OlQ9N2F-
SKBR3	M1;qdWN6fG:2b4jpZ4l1gSCjc4PhfS=>		MmTnO\|IhcHK\|	MXHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT2JTOyClZXzsd{Bi\nSncjC3NkBpenNuIFnDOVA:OC5yNUlOwG0v	NXj3[mQ4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmyN\|E5PjRpPkG5NlMyQDZ2PD;hQi=>
MCF7	NGr3dWFEgXSxdH;4bYNqfHliYYPzZZk>		MXm3NkBpenN?	MlnLR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{Bi\nSncjC3NkBpenNuIFnDOVA:OC5yN{JOwG0v	Ml7HQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl{M{G4OlQoRjF7MkOxPFY1RC:jPh?=
SKOV3	M1\BUGN6fG:2b4jpZ4l1gSCjc4PhfS=>		MUO3NkBpenN?	NEPVZY5EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUU0:YMzDj[YxteyCjZoTldkA4OiCqcoOsJGlEPTB;MD6xNlLPxE1w	NIXqWmo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUKzNVg3PCd-MUmyN\|E5PjR:L3G+
SKBR3	NIGyWGpEgXSxdH;4bYNqfHliYYPzZZk>		NH31WWY4OiCqcoO=	Mlj3R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2tDWjNiY3XscJMh[W[2ZYKgO\|IhcHK\|IHnuJJBz\XOnbnPlJI9nKE6TT{GgbY5pcWKrdH;yJIRq[2:3bXHyc4wtKEmFNUC9NE4zO87:TT6=	MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTJ\|MUi2OEc,OTl{M{G4OlQ9N2F-
MCF7	M2rVfWN6fG:2b4jpZ4l1gSCjc4PhfS=>		MVO3NkBpenN?	NIPQU5FEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGGodHXyJFczKGi{czDpckBxemW\|ZX7j[UBw\iCQUV:xJIlvcGmkaYTvdkBlcWOxdX3hdo9tNCCLQ{WwQVAvQDZ{zszNMi=>	MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTJ\|MUi2OEc,OTl{M{G4OlQ9N2F-
NCI-H596	MkLKR5l1d3SxeHnjbZR6KGG\|c3H5		MnHaO\|IhcHK\|	MWnDfZRwfG:6aXPpeJkh[WejaX7zeEBPWTBzLXTl[olkcWWwdDDoeY1idiCQQ1mtTFU6PiClZXzsd{Bi\nSncjC3NkBpenNuIFnDOVA:OS5zzszNMi=>	M1Tv[\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MkOxPFY1Lz5zOUKzNVg3PDxxYU6=
MDA468	M1LoemN6fG:2b4jpZ4l1gSCjc4PhfS=>		Mn:1O\|IhcHK\|	M1:0[GN6fG:2b4jpZ4l1gSCjZ3HpcpN1KE6TMEGt[IVncWOrZX70JIh2dWGwIF3ERVQ3QCClZXzsd{Bi\nSncjC3NkBpenNuIFnDOVA:OS54zszNMi=>	M{W0N\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MkOxPFY1Lz5zOUKzNVg3PDxxYU6=
SKBR3	NXLpeFBNS3m2b4TvfIlkcXS7IHHzd4F6		MknZO\|IhcHK\|	NEjC[pREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUU0KUMzDj[YxteyCjZoTldkA4OiCqcoOgZpkh[2WubITpeIVzNWeubzDhd5NigSxiSVO1NF0xNjB{NN88UU4>	Mnu4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl2MEW1NlgoRjF7NEC1OVI5RC:jPh?=
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Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID

Western blot	HSP90 / HSP70 ; p-Akt / Survivin / MMP2 ; PARP / Cleaved caspase-3 / Cleaved caspase-8 / Cleaved caspase-9 / PUMA ; p-ALK / ALK / p-Akt / Akt / p-ERK / ERK ; α-Tax / α-IKKα / α-IKKβ/ α-NEMO / α-TBK1 / α-p65 / α-p50	28915605 26219569 24109220
Growth inhibition assay	Cell proliferation	28915605

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. ^[2] 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. ^[4] 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. ^[5]

Protocol (from reference)

Kinase Assay:^[1]	Fluorescence polarization (FP)-based competition binding assay: This assay utilizes a boron difluoride dipyrromethene (BODIPY) labeled geldanamycin analogue (BODIPY-AG) as a probe and measured fluorescence polarization upon binding of the probe to a protein. Native human Hsp90 protein (α + β isoforms) is isolated from HeLa cells. BODIPY-AG solution is freshly prepared in FP assay buffer (20 mM HEPES-KOH, pH 7.3, 1.0 mM EDTA, 100 mM KCl, 5.0 mM MgCl₂, 0.01% NP-40, 0.1 mg/mL fresh bovine γ-globulin (BGG), 1.0 mM fresh DTT, and protease inhibitor from stock solution in DMSO. Competition curves are obtained by mixing 10 μL each of a solution containing BODIPY-AG and Hsp90, and a serial dilution of 17-DMAG freshly prepared in FP assay buffer from stock solution in DMSO. Final concentrations are 10 nM BODIPY-AG, 40 or 60 nM Hsp90, varying concentration of 17-DMAG (0.10 nM-10 μM), and ≤0.25% DMSO in a 384-well microplate. After 3 hours incubation at 30 °C, fluorescence anisotropy (γ_Ex = 485 nm, γ_Em = 535 nm) is measured on an EnVision 2100 multilabel plate reader. IC50 value of 17-DMAG is obtained from the competition curves.
Cell Research:^[5]	Cell lines: Chronic lymphocytic leukemia (CLL) Concentrations: Dissolved in DMSO, final concentrations ~1 μM Incubation Time: 24, or 48 hours Method: Cells are exposed to various concentrations of 17-DMAG for 24, or 48 hours. For the assessment of cytotoxicity, MTT reagent is then added, and plates are incubated for an additional 24 hours before spectrophotometric measurement. Apoptosis is determined by staining with annexin V-fluorescein isothiocyanate and propidium iodide (PI). (Only for Reference)
Animal Research:^[5]	Animal Models: SCID mice engrafted with TCL1 leukemia cells Dosages: 10 mg/kg Administration: Intraperitoneal injection 5 times per week (Only for Reference)

References

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Solubility (25°C)

In vitro	DMSO	131 mg/mL (200.54 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	Add solvents to the product individually and in order (Data is from Selleck tests instead of citations): 1% DMSO+30% polyethylene glycol+1% Tween 80 For best results, use promptly after mixing. Click to purchase: Tween 80	30 mg/mL

* 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	653.21
Formula	C₃₂H₄₈N₄O₈•HCl
CAS No.	467214-21-7
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CC1CC(C(C(C=C(C(C(C=CC=C(C(=O)NC2=CC(=O)C(=C(C1)C2=O)NCCN(C)C)C)OC)OC(=O)N)C)C)O)OC.Cl

Download Alvespimycin (17-DMAG) HCl SDF

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Dilution Calculator Molecular Weight Calculator

Clinical Trial Information

NCT Number	Recruitment	Interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT00780000	Terminated	Drug: Alvespimycin	Breast Cancer	Bristol-Myers Squibb	April 2008	Phase 2
NCT00248521	Unknown status	Drug: alvespimycin hydrochloride	Unspecified Adult Solid Tumor Protocol Specific	Institute of Cancer Research United Kingdom\|National Cancer Institute (NCI)	October 2005	Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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.

Handling Instructions

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