Retaspimycin

"目錄號(hào): HY-15263

Cell Cycle/DNA DamageMetabolic Enzyme/Protease-

Retaspimycin(IPI 504)是HSP90抑制劑,具有抗增殖和抗腫瘤活性弹惦。

HSP

相關(guān)產(chǎn)品

17-AAG-Triptolide-NVP-AUY922-Ganetespib-Geldanamycin-Teprenone-Rocaglamide-VER-155008-AT13387-Retaspimycin Hydrochloride-Alvespimycin hydrochloride-Debio 0932-BIIB021-PU-H71-NVP-HSP990-

生物活性

Description

Retaspimycin(IPI 504) is a small-molecule inhibitor of heat shock protein 90 (HSP90) with antiproliferative and antineoplastic activities. IC50 Value:Target: HSPRetaspimycin binds to and inhibits the cytosolic chaperone functions of HSP90, which maintains the stability and functional shape of many oncogenic signaling proteins and may be overexpressed or overactive in tumor cells. Retaspimycin-mediated inhibition of HSP90 promotes the proteasomal degradation of oncogenic signaling proteins in susceptible tumor cell populations, which may result in the induction of apoptosis.

Clinical Trial

NCT01362400

Infinity Pharmaceuticals, Inc.

Non Small Cell Lung Cancer

May 2011

Phase 2

NCT00564928

Infinity Pharmaceuticals, Inc.

Prostate Cancer-Prostatic Neoplasms-Cancer of the Prostate

November 2007

Phase 2

NCT00606814

Infinity Pharmaceuticals, Inc.

Solid Tumors

December 2007

Phase 1

NCT00113204

Infinity Pharmaceuticals, Inc.

Multiple Myeloma

June 2005

Phase 1

NCT00817362

Infinity Pharmaceuticals, Inc.

Breast Cancer-HER2 Positive Breast Cancer-Metastatic Breast Cancer-Cancer of the Breast

March 2009

Phase 2

NCT00627419

Infinity Pharmaceuticals, Inc.

Metastatic Melanoma

February 2008

Phase 2

NCT00276302

Infinity Pharmaceuticals, Inc.

Gastrointestinal Stromal Tumors-Soft Tissue Sarcomas

December 2005

Phase 1

NCT00627627

MedImmune LLC

Breast Cancer

April 2008

Phase 1-Phase 2

NCT00969917

Infinity Pharmaceuticals, Inc.

Dedifferentiated Liposarcoma

January 2010

Phase 2

NCT01427946

Infinity Pharmaceuticals, Inc.

Non-small Cell Lung Cancer

July 2011

Phase 1-Phase 2

NCT00431015

Infinity Pharmaceuticals, Inc.

Lung Cancer

January 2007

Phase 1-Phase 2

NCT00688766

Infinity Pharmaceuticals, Inc.-MedImmune LLC-AstraZeneca

Gastrointestinal Stromal Tumors

August 2008

Phase 3

NCT01228435

Massachusetts General Hospital-Dana-Farber Cancer Institute-Infinity Pharmaceuticals, Inc.

Lung Cancer-Stage IIIb Lung Cancer-Stage IV Lung Cancer

October 2010

Phase 2

View MoreCollapse

References

[1].Oh WK, Galsky MD, Stadler WM, Srinivas S, Chu F, Bubley G, Goddard J, Dunbar J, Ross RW.Multicenter phase II trial of the heat shock protein 90 inhibitor, retaspimycin hydrochloride (IPI-504), in patients with castration-resistant prostate cancer.? Urolog

[2].Hanson BE, Vesole DH.? Retaspimycin hydrochloride (IPI-504): a novel heat shock protein inhibitor as an anticancer agent.? Expert Opin Investig Drugs. 2009 Sep;18(9):1375-83.

[3].Siegel D, Jagannath S, Vesole DH, Borello I, Mazumder A, Mitsiades C, Goddard J, Dunbar J, Normant E, Adams J, Grayzel D, Anderson KC, Richardson P.? A phase 1 study of IPI-504 (retaspimycin hydrochloride) in patients with relapsed or relapsed and refract

[4].The antiproliferative activity of the heat shock protein 90 inhibitor IPI-504 is not dependent on NAD(P)H:quinone oxidoreductase 1 activity in vivo By Douglas, Mark; Lim, Alice R.; Porter, James R.; West, Kip; Pink, Melissa M.; Ge, Jie; Wylie, Andrew A.;

[5].A mechanistic and structural analysis of the inhibition of the 90-kDa heat shock protein by the benzoquinone and hydroquinone ansamycins By Reigan, Philip; Siegel, David; Guo, Wenchang; Ross, David From Molecular Pharmacology (2011), 79(5), 823-832.

?著作權(quán)歸作者所有,轉(zhuǎn)載或內(nèi)容合作請(qǐng)聯(lián)系作者
  • 序言:七十年代末尚镰,一起剝皮案震驚了整個(gè)濱河市院仿,隨后出現(xiàn)的幾起案子纵搁,更是在濱河造成了極大的恐慌拓哟,老刑警劉巖主到,帶你破解...
    沈念sama閱讀 222,252評(píng)論 6 516
  • 序言:濱河連續(xù)發(fā)生了三起死亡事件,死亡現(xiàn)場(chǎng)離奇詭異阴挣,居然都是意外死亡气堕,警方通過查閱死者的電腦和手機(jī),發(fā)現(xiàn)死者居然都...
    沈念sama閱讀 94,886評(píng)論 3 399
  • 文/潘曉璐 我一進(jìn)店門畔咧,熙熙樓的掌柜王于貴愁眉苦臉地迎上來茎芭,“玉大人,你說我怎么就攤上這事誓沸∶纷” “怎么了?”我有些...
    開封第一講書人閱讀 168,814評(píng)論 0 361
  • 文/不壞的土叔 我叫張陵拜隧,是天一觀的道長(zhǎng)宿百。 經(jīng)常有香客問我,道長(zhǎng)洪添,這世上最難降的妖魔是什么犀呼? 我笑而不...
    開封第一講書人閱讀 59,869評(píng)論 1 299
  • 正文 為了忘掉前任,我火速辦了婚禮薇组,結(jié)果婚禮上,老公的妹妹穿的比我還像新娘坐儿。我一直安慰自己律胀,他們只是感情好,可當(dāng)我...
    茶點(diǎn)故事閱讀 68,888評(píng)論 6 398
  • 文/花漫 我一把揭開白布貌矿。 她就那樣靜靜地躺著炭菌,像睡著了一般。 火紅的嫁衣襯著肌膚如雪逛漫。 梳的紋絲不亂的頭發(fā)上黑低,一...
    開封第一講書人閱讀 52,475評(píng)論 1 312
  • 那天,我揣著相機(jī)與錄音,去河邊找鬼克握。 笑死蕾管,一個(gè)胖子當(dāng)著我的面吹牛,可吹牛的內(nèi)容都是我干的菩暗。 我是一名探鬼主播掰曾,決...
    沈念sama閱讀 41,010評(píng)論 3 422
  • 文/蒼蘭香墨 我猛地睜開眼,長(zhǎng)吁一口氣:“原來是場(chǎng)噩夢(mèng)啊……” “哼停团!你這毒婦竟也來了旷坦?” 一聲冷哼從身側(cè)響起,我...
    開封第一講書人閱讀 39,924評(píng)論 0 277
  • 序言:老撾萬榮一對(duì)情侶失蹤佑稠,失蹤者是張志新(化名)和其女友劉穎秒梅,沒想到半個(gè)月后,有當(dāng)?shù)厝嗽跇淞掷锇l(fā)現(xiàn)了一具尸體舌胶,經(jīng)...
    沈念sama閱讀 46,469評(píng)論 1 319
  • 正文 獨(dú)居荒郊野嶺守林人離奇死亡捆蜀,尸身上長(zhǎng)有42處帶血的膿包…… 初始之章·張勛 以下內(nèi)容為張勛視角 年9月15日...
    茶點(diǎn)故事閱讀 38,552評(píng)論 3 342
  • 正文 我和宋清朗相戀三年,在試婚紗的時(shí)候發(fā)現(xiàn)自己被綠了辆琅。 大學(xué)時(shí)的朋友給我發(fā)了我未婚夫和他白月光在一起吃飯的照片漱办。...
    茶點(diǎn)故事閱讀 40,680評(píng)論 1 353
  • 序言:一個(gè)原本活蹦亂跳的男人離奇死亡,死狀恐怖婉烟,靈堂內(nèi)的尸體忽然破棺而出娩井,到底是詐尸還是另有隱情,我是刑警寧澤似袁,帶...
    沈念sama閱讀 36,362評(píng)論 5 351
  • 正文 年R本政府宣布洞辣,位于F島的核電站,受9級(jí)特大地震影響昙衅,放射性物質(zhì)發(fā)生泄漏扬霜。R本人自食惡果不足惜,卻給世界環(huán)境...
    茶點(diǎn)故事閱讀 42,037評(píng)論 3 335
  • 文/蒙蒙 一而涉、第九天 我趴在偏房一處隱蔽的房頂上張望著瓶。 院中可真熱鬧,春花似錦啼县、人聲如沸材原。這莊子的主人今日做“春日...
    開封第一講書人閱讀 32,519評(píng)論 0 25
  • 文/蒼蘭香墨 我抬頭看了看天上的太陽余蟹。三九已至,卻和暖如春子刮,著一層夾襖步出監(jiān)牢的瞬間威酒,已是汗流浹背。 一陣腳步聲響...
    開封第一講書人閱讀 33,621評(píng)論 1 274
  • 我被黑心中介騙來泰國(guó)打工, 沒想到剛下飛機(jī)就差點(diǎn)兒被人妖公主榨干…… 1. 我叫王不留葵孤,地道東北人担钮。 一個(gè)月前我還...
    沈念sama閱讀 49,099評(píng)論 3 378
  • 正文 我出身青樓,卻偏偏與公主長(zhǎng)得像佛呻,于是被迫代替她去往敵國(guó)和親裳朋。 傳聞我的和親對(duì)象是個(gè)殘疾皇子,可洞房花燭夜當(dāng)晚...
    茶點(diǎn)故事閱讀 45,691評(píng)論 2 361

推薦閱讀更多精彩內(nèi)容