Geldanamycin | NSC 122750 | Hsp90 Inhibitor | AmBeed-信号通路专用抑制剂

首页 / / / / Geldanamycin

格尔德霉素 /Geldanamycin {[allProObj[0].p_purity_real_show]}

货号：A164935 同义名： NSC 122750

Geldanamycin是一种Hsp90抑制剂，对多种革兰氏阳性和一些革兰氏阴性细菌具有抗菌活性，还表现出抗流感病毒H5N1的活性。

Geldanamycin 化学结构
CAS号：30562-34-6

Geldanamycin 3D分子结构
CAS号：30562-34-6

规格	价格	会员价	库存	数量
{[ item.pr_size ]}	{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_am, item.pr_size) ]}	{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_am, item.pr_size) ]}	{[ getRatePrice(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_am, item.pr_size) ]}	{[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate) ]}	现货	咨询	- +

购物车0 收藏询单

sales@ambeed.cn tech@ambeed.cn 400-920-2911 产品手册产品订购技术咨询
快速发货顺丰冷链运输，1-2 天到达

品质保证

技术支持

免费溶解

Geldanamycin 纯度/质量文件产品仅供科研

货号：A164935 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell, 2024, 101755. Ambeed. [ A399663 ]; • EMBO J., 2024. Ambeed. [ A295334 ]; • JMC, 2024, 67(20): 18265-18289. Ambeed. [ A538667 , A341145 , A117430 , A172297 ]; • JMC, 2024. Ambeed. [ A210558 , A1518164 ]; • Cell Death Discov., 2024, 10, 436. Ambeed. [ A384235 ]; 更多 >

自噬亚型比较

产品名称	Autophagy ↓ ↑	其他靶点	纯度
SBI-0206965	+++ ULK1, IC50: 108 nM ULK2, IC50: 711 nM		97%
Hydroxychloroquine sulfate	✔		99%
Valproic acid sodium	✔	HDAC	97%
PFK-015	++ PFKFB3, IC50: 207 nM		99%+
MRT68921 hydrochloride	++++ ULK1, IC50: 2.9 nM ULK2, IC50: 1.1 nM		99%+
ROC-325	✔		99%+
Autophinib	+++ Autophagy, IC50: 40 nM		97%
Lys05	✔		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Geldanamycin 生物活性

描述

HSP90 (heat shock protein 90) is a cellular ubiquitous molecular chaperone responsible for promoting the conformational mutation and stabilization of several client oncoproteins, including Met, B-Raf, p53, Akt, and Kit, function of which is required by tumor cells to maintain appropriate client protein expression necessary for proliferation and survival. Geldanamycin is the first class of HSP90 inhibitor with a Kd value of 1.2 µM and IC50<2μM for ATPase activity of Hsp90^[1]. Treatment with geldanamycin at concentration of 0.5μM or 1μM for 24h reduced the protein level of AKT, as well as Raf-1 and its downstream p-MEK1/2, but not N-Ras or MEK1/2 in SH-SY5Y cells. Geldanamycin at concentration of 1μM for 48h could induce apoptosis in several neuroblastoma cell lines, including SH-SY5Y, SK-N-SH and LAN-1 cells^[2]. Intraperitoneal administration of geldanamycin (10 mg/kg) ameliorated ICH-induced increase of brain water content significantly, improved the neurological outcome and had a neuroprotective effect after ICH^[3].

作用机制

Geldanamycin can bind to the N-terminal ATP/ADP-binding domain of Hsp90 and minhibit the inherent ATPase activity of Hsp90.^[1]

Geldanamycin 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
A2780 cells		Proliferation assay		Compound was evaluated for antiproliferative activity against human ovarian carcinoma cell line A2780, IC50=3.4 μM	11514145
HCT116 cells		Proliferation assay		Antiproliferative activity against human HCT116 cells by luminescence assay, EC50=0.03 μM	21605975
HEK293T cells		Function assay		Inhibition of TNF-alpha-induced NF-kappaB activation expressed in HEK293T cells by luciferase reporter gene assay	18408713
HT-29 cell		Growth inhibition assay		Inhibitory concentration against human colorectal carcinoma HT-29 cell lines, IC50=24.5 nM	15658879

Geldanamycin 动物研究

Dose

Mice: 5 mg/kg - 20 mg/kg^[4] (i.p.), 0.1 mg/kg - 1 mg/kg^[5] (intraplantar)

Administration

i.p., intraplantar

Pharmacokinetics

Animal	Mice^[6]	Dogs^[6]
Administration	i.v.	i.v.
MRT	20.7 min	46.6 min
V_z		4.11 L/kg
V_z/F	3.81 L/kg
CL	30.5 ml/min/kg	49.4 ml/min/kg
Vss	0.68 L/kg	2.31 L/kg

Geldanamycin 临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01193491	Hematologic Malignancies	Phase 1	Terminated(Drug exposure of re... 展开 >>taspimycin HCl was superior to IPI-493, Infinity will focus on Retaspimycin HCL) 收起 <<	-	United States, Maryland ... 展开 >> 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 收起 <<
NCT00319930	Chronic Lymphocytic Leukemia	Phase 1	Terminated(Discontinuation of ... 展开 >>program) 收起 <<	-	United States, Florida ... 展开 >> 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 收起 <<
NCT00093821	Childhood Chronic Myelogenous ... 展开 >>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 收起 <<	Phase 1	Completed	-	United States, New York ... 展开 >> Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10065 收起 <<

Geldanamycin 参考文献

[1]Woodhead AJ, Angove H, et al. Discovery of (2,4-dihydroxy-5-isopropylphenyl)-[5-(4-methylpiperazin-1-ylmethyl)-1,3-dihydroisoindol-2-yl] methanone (AT13387), a novel inhibitor of the molecular chaperone Hsp90 by fragment based drug design. J Med Chem. 2010 Aug 26;53(16):5956-69.

[2]Kim S, Kang J, et al. Geldanamycin decreases Raf-1 and Akt levels and induces apoptosis in neuroblastomas. Int J Cancer. 2003 Jan 20;103(3):352-9.

[3]Manaenko A, Fathali N, et al. Geldanamycin reduced brain injury in mouse model of intracerebral hemorrhage. Acta Neurochir Suppl. 2011;111:161-5.

[4]Kasibhatla SR, Hong K, et al. Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity. J Med Chem. 2007 Jun 14;50(12):2767-78. Epub 2007 May 8.

[5]Bucci M, Roviezzo F, et al. Geldanamycin, an inhibitor of heat shock protein 90 (Hsp90) mediated signal transduction has anti-inflammatory effects and interacts with glucocorticoid receptor in vivo. Br J Pharmacol. 2000 Sep;131(1):13-6.

[6]Supko JG, Hickman RL, et al. Preclinical pharmacologic evaluation of geldanamycin as an antitumor agent. Cancer Chemother Pharmacol. 1995;36(4):305-15.

Geldanamycin 实验方案

计算器

存储液制备

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

Geldanamycin 技术信息

CAS号	30562-34-6
分子式	C₂₉H₄₀N₂O₉
分子量	560.636

别名	NSC 122750
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C

溶解度

DMSO: 25 mg/mL(44.59 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

A2780 cells	Proliferation assay		Compound was evaluated for antiproliferative activity against human ovarian carcinoma cell line A2780, IC50=3.4 μM	11514145
HCT116 cells	Proliferation assay		Antiproliferative activity against human HCT116 cells by luminescence assay, EC50=0.03 μM	21605975
HEK293T cells	Function assay		Inhibition of TNF-alpha-induced NF-kappaB activation expressed in HEK293T cells by luciferase reporter gene assay	18408713
HT-29 cell	Growth inhibition assay		Inhibitory concentration against human colorectal carcinoma HT-29 cell lines, IC50=24.5 nM	15658879
human A431 cells	Cytotoxic assay	72 h	Cytotoxicity against human A431 cells after 72 hrs by MTT assay, IC50=40 nM	25277067
human A431 cells	Proliferation assay	72 h	Antiproliferative activity against human A431 cells after 72 hrs, IC50=0.2 μM	20655237
human A549 cells	Growth inhibition assay		Growth inhibition of human A549 cells, GI50=64 nM	18243703
human A549 cells	Cytotoxic assay	72 h	Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50=97 nM	25277067
human A549 cells	Cytotoxic assay	2 days	Cytotoxicity against human A549 cells after 2 days by AlamarBlue assay, IC50=0.15 μM	23947794
human BGC823 cells	Cytotoxic assay	72 h	Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay, IC50=40 nM	25277067
human DLD1 cells	Growth inhibition assay		Growth inhibition of human DLD1 cells, GI50=37 nM	18243703
human HCT116 cells	Growth inhibition assay		Growth inhibition of human HCT116 cells, GI50=21 nM	18243703
human HeLa cells	Cytotoxic assay	72 h	Cytotoxicity against human HeLa cells after 72 hrs by MTT assay, IC50=0.798 μM	25277067
human HepG2 cells	Cytotoxic assay	72 h	Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, IC50=40 nM	25277067
human HepG2 cells	Cytotoxic assay		Cytotoxicity against human HepG2 cells by MTT assay, IC50=0.3 μM	23656556
human HL7702 cells	Cytotoxic assay	72 h	Cytotoxicity against human HL7702 cells after 72 hrs by MTT assay, IC50=0.141 μM	25277067
human Jurkat cells	Function assay		Inhibition of TNF-alpha-induced NF-kappaB activation expressed in FADD deficient human Jurkat cells by luciferase reporter gene assay	18408713
human LNCAP cells	Cytotoxic assay	72 h	Cytotoxicity against human LNCAP cells after 72 hrs by MTT assay, IC50=0.43 μM	25105924
human LS174T cells	Cytotoxic assay		Cytotoxicity against human LS174T cells by MTS assay, IC50=0.45 μM	17034135
human MCF7 cells	Cytotoxic assay		Cytotoxicity against human MCF7 cells by SRB assay, IC50=9.6 μM	19560353
human MCF7 cells	Growth inhibition assay		Growth inhibition of human MCF7 cells after days by SRB assay, GI50=35.6 μM	17869098
human MDA-MB-231 cells	Cytotoxic assay	72 h	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50=50 nM	25277067
human SKBR3 cells	Cytotoxic assay	72 h	Cytotoxicity against human SKBR3 cells after 72 hrs by celltiter-glo assay, IC50=41 nM	19405528
human SKBR3 cells	Function assay	24 h	Inhibition of Hsp90-mediated HER2 degradation in human SKBR3 cells after 24 hrs by Western blot	18816111
human SK-BR-3 cells	Proliferation assay		Antiproliferative activity against human SK-BR-3 cells, IC50=15.8 nM	19896848
human SW480 cells	Cytotoxic assay	72 h	Cytotoxicity against human SW480 cells after 72 hrs by MTT assay, IC50=0.31 μM	25277067
human U87MG cells	Proliferation assay		Antiproliferative activity against human U87MG cells, IC50=89 nM	21715165
HUVEC cells	Cytotoxic assay	72 h	Cytotoxicity against HUVEC cells after 72 hrs by MTT assay, IC50=19 nM	25277067
K562 cell	Growth inhibition assay		Inhibitory concentration against human leukemia K562 cell lines, IC50=22.1 nM	15658879
MCF-7 cell	Growth inhibition assay		Inhibitory concentration against human breast cancer MCF-7 cell lines, IC50=6.5 nM	15658879
MCF7 cells	Proliferation assay	72 h	Antiproliferative activity against human MCF7 cells expressing estrogen receptor after 72 hrs, IC50=9.8 nM	23648180
MDA-kb2 cells	Function assay	18 h	Inhibition of HSP90 in human MDA-kb2 cells assessed as reduction in glucocorticoid receptor-dependent luciferase expression after 18 hrs by firefly luciferase reporter gene assay, IC50=10 nM	24984936
mouse P19 cells	Cytotoxic assay	18 h	Cytotoxicity against mouse P19 cells after 18 hrs, IC50=0.1 μM	17442565
NCI-H1975 cells	Proliferation assay		Antiproliferative activity against human NCI-H1975 cells, IC50=36 nM	21715165
rat L6 cells	Cytotoxic assay	72 h	Cytotoxicity against rat L6 cells after 72 hrs by Alamar Blue assay, IC50=5 μM	24580531
Sf9 cells	Function assay		Displacement of GM-BODIPY from human full length HSP90 alpha expressed in baculovirus-infected Sf9 cells after 16 hrs by fluorescence polarization assay, IC50=74 nM	24751441
SKBR3 cells	Proliferation assay	72 h	Antiproliferative activity against estrogen receptor deficient human SKBR3 cells after 72 hrs, IC50=8.5 nM	23648180
SW620 cell	Growth inhibition assay		Inhibitory concentration against human colorectal carcinoma SW620 cell lines, IC50=6.2 nM	15658879

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT01193491	Hematologic Malignancies	Phase 1	Terminated(Drug exposure of re... 展开 >>taspimycin HCl was superior to IPI-493, Infinity will focus on Retaspimycin HCL) 收起 <<	-	United States, Maryland ... 展开 >> 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 收起 <<
NCT00319930	Chronic Lymphocytic Leukemia	Phase 1	Terminated(Discontinuation of ... 展开 >>program) 收起 <<	-	United States, Florida ... 展开 >> 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 收起 <<
NCT00093821	Childhood Chronic Myelogenous ... 展开 >>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 收起 <<	Phase 1	Completed	-	United States, New York ... 展开 >> Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10065 收起 <<
NCT00119236	Unspecified Adult Solid Tumor,... 展开 >> Protocol Specific 收起 <<	Phase 1	Completed	-	United States, New York ... 展开 >> Memorial Sloan Kettering Cancer Center New York, New York, United States, 10065 收起 <<
NCT00087386	Recurrent Melanoma ... 展开 >> Stage III Melanoma Stage IV Melanoma 收起 <<	Phase 2	Terminated	-	United States, New York ... 展开 >> Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10065 收起 <<
NCT00058253	Recurrent Prostate Cancer ... 展开 >> Stage IV Prostate Cancer Unspecified Adult Solid Tumor, Protocol Specific 收起 <<	Phase 1	Completed	-	United States, New York ... 展开 >> Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10065 收起 <<
NCT00004065	Bladder Cancer ... 展开 >> 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 收起 <<	Phase 1	Completed	-	United States, California ... 展开 >> 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 收起 <<
NCT00093405	Kidney Cancer	Phase 2	Completed	-	United States, New York ... 展开 >> Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10021 收起 <<
NCT00003969	Unspecified Adult Solid Tumor,... 展开 >> Protocol Specific 收起 <<	Phase 1	Completed	-	United Kingdom ... 展开 >> Royal Marsden NHS Foundation Trust - London London, England, United Kingdom, SW3 6JJ 收起 <<
NCT00019708	Extranodal Marginal Zone B-cel... 展开 >>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 收起 <<	Phase 1	Terminated	-	United States, Nebraska ... 展开 >> University of Nebraska Medical Center Omaha, Nebraska, United States, 68198 收起 <<

格尔德霉素 /Geldanamycin {[allProObj[0].p_purity_real_show]}

Geldanamycin 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Geldanamycin 质控信息

Geldanamycin 生物活性

Geldanamycin 细胞研究

Geldanamycin 动物研究

Geldanamycin 临床研究

Geldanamycin 参考文献

Geldanamycin 实验方案

Geldanamycin 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

格尔德霉素 /Geldanamycin {[allProObj[0].p_purity_real_show]}

Geldanamycin 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Geldanamycin 质控信息

Geldanamycin 生物活性

Geldanamycin 细胞研究

Geldanamycin 动物研究

Geldanamycin 临床研究

Geldanamycin 参考文献

Geldanamycin 实验方案

Geldanamycin 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

请登录您的专属账户

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

Geldanamycin 纯度/质量文件产品仅供科研