Tanespimycin (坦螺旋霉素）

Tanespimycin (17-AAG) 是有效的 HSP90 抑制劑，IC50 為 5 nM，對腫瘤細胞 HSP90 的親和性比正常細胞高 100 倍。Tanespimycin 消耗細胞內(nèi) STK38/NDR1，并降低 STK38 激酶活性。Tanespimycin 還下調(diào) stk38 基因表達。貨號：HY-10211 ，CAS：75747-14-7

參數(shù)品牌：MCE

產(chǎn)品參數(shù)

品牌：MCE

型號：HY-10211

起訂量：1

規(guī)格:：10mg

價格:：￥700

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Tanespimycin (Synonyms: 坦螺旋霉素; 17-AAG; NSC 330507; CP 127374)

Tanespimycin (17-AAG) 是有效的 HSP90 抑制劑，IC₅₀ 為 5 nM，對腫瘤細胞 HSP90 的親和性比正常細胞高 100 倍。Tanespimycin 消耗細胞內(nèi) STK38/NDR1，并降低 STK38 激酶活性。Tanespimycin 還下調(diào) stk38 基因表達。

生物活性

Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an IC₅₀ of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90^[1]^[5]. Tanespimycin depletes cellular STK38/NDR1 and reduces STK38 kinase activity. Tanespimycin also downregulates the stk38 gene expression^[3].

體外研究(In Vitro)

Tanespimycin causes the degradation of HER2, Akt, and both mutant and wild-type AR and the retinoblastoma-dependent G1 growth arrest of prostate cancer cells. Tanespimycin inhibits prostate cancer cell lines with IC₅₀s ranged from 25-45 nM (LNCaP, 25 nM; LAPC-4, 40 nM; DU-145, 45 nM; and PC-3, 25 nM)^[1].
Tanespimycin (0.1-1 μM) induces a nearly complete loss of ErbB2 on ErbB2-overexpressing breast cancer cells^[2]. Tanespimycin inhibits cell growth and induces G2/M cell cycle arrest and apoptosis in CCA cells together with the down-regulation of Bcl-2, Survivin and Cyclin B1, and the up-regulation of cleaved PARP^[3].

體內(nèi)研究(In Vivo)

Tanespimycin (25-200 mg/kg, i.p.) causes a dose-dependent decline in AR, HER2, and Akt expression in prostate cancer xenografts. Tanespimycin treatment at doses sufficient to induce AR, HER2, and Akt degradation results in the dose-dependent inhibition of androgen-dependent and -independent prostate cancer xenograft growth without toxicity^[1].
Tanespimycin (60 mg/kg) with Rapamycin (30 mg/kg) inhibits A549 and MDA-MB-231 tumor growth and effects tumor cures in MDA-MB-231 tumor-bearing animals by tail vein injection^[4].

分子量:585.69

Formula:C₃₁H₄₃N₃O₈

CAS 號:75747-14-7

中文名稱:坦螺旋霉素

運輸條件:Room temperature in continental US; may vary elsewhere.

儲存方式:

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性數(shù)據(jù)

In Vitro:

DMSO : 50 mg/mL (85.37 mM; Need ultrasonic)

配制儲備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	1.7074 mL	8.5369 mL	17.0739 mL
5 mM	0.3415 mL	1.7074 mL	3.4148 mL
10 mM	0.1707 mL	0.8537 mL	1.7074 mL

*

請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。

In Vivo:

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：

——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

1.

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 5 mg/mL (8.54 mM); Clear solution
2.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 5 mg/mL (8.54 mM); Clear solution
3.

請依序添加每種溶劑： 15% Cremophor EL 85% Saline
Solubility: 5 mg/mL (8.54 mM); Suspended solution; Need ultrasonic
4.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 1.62 mg/mL (2.77 mM); Clear solution

參考文獻

[1]. Solit DB, et al. 17-Allylamino17-demethoxygeldanamycin induces the degradation of androgen receptor and HER-2/neu and inhibits the growth of prostate cancer xenografts.Clin Cancer Res, 2002, 8(5), 986-993.

[2]. Raja, Srikumar M., et al. 17-AAG induces enhanced ubiquitinylation and lysosomal pathway-dependent ErbB2 degradation and cytotoxicity in ErbB2-overexpressing breast cancer cells. Cancer Biology & Therapy (2008), 7(10), 163

[3]. Zhang J, et al. The heat shock protein 90 inhibitor 17-AAG suppresses growth and induces apoptosis in human cholangiocarcinoma cells.Clin Exp Med. 2012 Sep 7.

[4]. Newman B, et al. HSP90 Inhibitor 17-AAG Selectively Eradicates Lymphoma Stem Cells.Cancer Res. 2012 Sep 1;72(17):4551-61. Epub 2012 Jun 29.

[5]. Kamal A, et al. A high-affinity conformation of Hsp90 confers tumour selectivity on Hsp90 inhibitors. Nature. 2003 Sep 25;425(6956):407-10.

[6]. Enomoto A, et al. The HSP90 inhibitor 17-allylamino17-demethoxygeldanamycin modulates radiosensitivity by downregulating serine/threonine kinase 38 via Sp1 inhibition. Eur J Cancer. 2013 Nov;49(16):3547-58.

Tanespimycin (坦螺旋霉素）

Tanespimycin (17-AAG) 是有效的 HSP90 抑制劑，IC50 為 5 nM，對腫瘤細胞 HSP90 的親和性比正常細胞高 100 倍。Tanespimycin 消耗細胞內(nèi) STK38/NDR1，并降低 STK38 激酶活性。Tanespimycin 還下調(diào) stk38 基因表達。貨號：HY-10211 ，CAS：75747-14-7

品牌：MCE

型號：HY-10211

起訂量：1

規(guī)格:：10mg

價格:：￥700

15906629305

在線客服

客服一

產(chǎn)品詳情

Tanespimycin (Synonyms: 坦螺旋霉素; 17-AAG; NSC 330507; CP 127374)

Tanespimycin (17-AAG) 是有效的 HSP90 抑制劑，IC₅₀ 為 5 nM，對腫瘤細胞 HSP90 的親和性比正常細胞高 100 倍。Tanespimycin 消耗細胞內(nèi) STK38/NDR1，并降低 STK38 激酶活性。Tanespimycin 還下調(diào) stk38 基因表達。

生物活性

Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an IC₅₀ of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90^[1]^[5]. Tanespimycin depletes cellular STK38/NDR1 and reduces STK38 kinase activity. Tanespimycin also downregulates the stk38 gene expression^[3].

體外研究(In Vitro)

Tanespimycin causes the degradation of HER2, Akt, and both mutant and wild-type AR and the retinoblastoma-dependent G1 growth arrest of prostate cancer cells. Tanespimycin inhibits prostate cancer cell lines with IC₅₀s ranged from 25-45 nM (LNCaP, 25 nM; LAPC-4, 40 nM; DU-145, 45 nM; and PC-3, 25 nM)^[1].
Tanespimycin (0.1-1 μM) induces a nearly complete loss of ErbB2 on ErbB2-overexpressing breast cancer cells^[2]. Tanespimycin inhibits cell growth and induces G2/M cell cycle arrest and apoptosis in CCA cells together with the down-regulation of Bcl-2, Survivin and Cyclin B1, and the up-regulation of cleaved PARP^[3].

體內(nèi)研究(In Vivo)

Tanespimycin (25-200 mg/kg, i.p.) causes a dose-dependent decline in AR, HER2, and Akt expression in prostate cancer xenografts. Tanespimycin treatment at doses sufficient to induce AR, HER2, and Akt degradation results in the dose-dependent inhibition of androgen-dependent and -independent prostate cancer xenograft growth without toxicity^[1].
Tanespimycin (60 mg/kg) with Rapamycin (30 mg/kg) inhibits A549 and MDA-MB-231 tumor growth and effects tumor cures in MDA-MB-231 tumor-bearing animals by tail vein injection^[4].

分子量:585.69

Formula:C₃₁H₄₃N₃O₈

CAS 號:75747-14-7

中文名稱:坦螺旋霉素

運輸條件:Room temperature in continental US; may vary elsewhere.

儲存方式:

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性數(shù)據(jù)

In Vitro:

DMSO : 50 mg/mL (85.37 mM; Need ultrasonic)

配制儲備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	1.7074 mL	8.5369 mL	17.0739 mL
5 mM	0.3415 mL	1.7074 mL	3.4148 mL
10 mM	0.1707 mL	0.8537 mL	1.7074 mL

*

請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。

In Vivo:

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：

——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

1.

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 5 mg/mL (8.54 mM); Clear solution
2.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 5 mg/mL (8.54 mM); Clear solution
3.

請依序添加每種溶劑： 15% Cremophor EL 85% Saline
Solubility: 5 mg/mL (8.54 mM); Suspended solution; Need ultrasonic
4.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 1.62 mg/mL (2.77 mM); Clear solution