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Venetoclax (維奈妥拉)

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Venetoclax (ABT-199; GDC-0199) 是一種高效,有選擇性和口服有效的 Bcl-2 抑制劑,Ki 小于0.01 nM。Venetoclax 可以誘導(dǎo)自噬 (autophagy) 作用。

貨號(hào):HY-15531
CAS:1257044-40-8
參數(shù)品牌:MCE
產(chǎn)品參數(shù)
品牌:MCE
型號(hào):HY-15531
起訂量:1
規(guī)格::2mg
價(jià)格::¥600
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產(chǎn)品詳情

Venetoclax (Synonyms: 維奈妥拉)

Venetoclax (ABT-199; GDC-0199) 是一種高效,有選擇性和口服有效的 Bcl-2 抑制劑,Ki 小于0.01 nM。Venetoclax 可以誘導(dǎo)自噬 (autophagy) 作用。


生物活性

Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy


體外研究(In Vitro)

Venetoclax (ABT-199) potently kills FL5.12-BCL-2 cells (EC50=4 nM), Venetoclax (ABT-199) shows much weaker activity against FL5.12-BCL-XL cells (EC50=261 nM). ABT-199 also shows selectivity in cellular mammalian two-hybrid assays, where it disrupts BCL-2-BIM complexes (EC50=3 nM) but is much less effective against BCL-XL-BCL-XS (EC50=2.2 μM) or MCL-1-NOXA complexes[


體內(nèi)研究(In Vivo)

After a single oral dose of 12.5 mg per kg body weight in xenografts derived from RS4;11 cells (ALL), Venetoclax (ABT-199) causes a maximal tumor growth inhibition (TGImax) of 47% (P<0.001) and tumor growth delay (TGD) of 26% (P<0.05)[1].
Treatment of established xenografted (a mouse xenograft model of the T-ALL cell line LOUCY) tumors with Venetoclax (ABT-199) 100 mg/kg for 4 days results in a significant reduction of leukemic burden


Clinical Trial

NCT NumberSponsorConditionStart DatePhase
NCT04282811Gruppo Italiano Malattie EMatologiche dell′Adulto
Chronic Lymphocytic Leukemia|Relapse Leukemia|Refractory Leukemia
July 24, 2020
NCT03112174Pharmacyclics LLC.|Janssen Research & Development, LLC
Mantle-Cell Lymphoma
May 12, 2017Phase 3
NCT03343678Boehringer Ingelheim
Leukemia, Lymphocytic, Chronic, B-Cell
January 17, 2018Phase 1



分子量:868.44


Formula:C45H50ClN7O7S


CAS 號(hào):1257044-40-8


中文名稱:維奈妥拉


運(yùn)輸條件:Room temperature in continental US; may vary elsewhere.


儲(chǔ)存方式:

Powder-20°C3 years

4°C2 years
In solvent-80°C6 months

-20°C1 month


溶解性數(shù)據(jù)


DMSO : 77.5 mg/mL (89.24 mM; Need ultrasonic)

Ethanol : < 1 mg/mL (insoluble)

配制儲(chǔ)備液
濃度溶劑體積質(zhì)量1 mg5 mg10 mg
1 mM1.1515 mL5.7575 mL11.5149 mL
5 mM0.2303 mL1.1515 mL2.3030 mL
10 mM0.1151 mL0.5757 mL1.1515 mL
*

請(qǐng)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(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 儲(chǔ)存時(shí),請(qǐng)?jiān)?6 個(gè)月內(nèi)使用,-20°C 儲(chǔ)存時(shí),請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。

In Vivo:

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

——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)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(qǐng)依序添加每種溶劑: 60% phosal 50 propylene glycol (PG), 30% polyethylene glycol 400 (PEG400), 10% ethanol

    Solubility: 20 mg/mL (23.03 mM); Suspended solution; Need ultrasonic


  • 2.


    請(qǐng)依序添加每種溶劑: 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 5.25 mg/mL (6.05 mM); Clear solution


  • 3.


    請(qǐng)依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.58 mg/mL (2.97 mM); Clear solution


  • 4.


    請(qǐng)依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (2.88 mM); Suspended solution; Need ultrasonic and warming


參考文獻(xiàn)

[1]. Souers AJ, et al. ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets. Nat Med. 2013 Feb;19(2):202-8.

[2]. Peirs S, et al. ABT-199 mediated inhibition of BCL-2 as a novel therapeutic strategy in T-cell acute lymphoblastic leukemia. Blood. 2014 Dec 11;124(25):3738-47.

[3]. Bi C, et al. Inhibition of 4EBP phosphorylation mediates the cytotoxic effect of mechanistic target of rapamycin kinase inhibitors in aggressive B-cell lymphomas. Haematologica. 2017 Apr;102(4):755-764.


Venetoclax (維奈妥拉)

Venetoclax (維奈妥拉)

分享到微信

×
Venetoclax (ABT-199; GDC-0199) 是一種高效,有選擇性和口服有效的 Bcl-2 抑制劑,Ki 小于0.01 nM。Venetoclax 可以誘導(dǎo)自噬 (autophagy) 作用。

貨號(hào):HY-15531
CAS:1257044-40-8
品牌:MCE
型號(hào):HY-15531
起訂量:1
規(guī)格::2mg
價(jià)格::¥600
15906629305
在線客服
產(chǎn)品詳情

Venetoclax (Synonyms: 維奈妥拉)

Venetoclax (ABT-199; GDC-0199) 是一種高效,有選擇性和口服有效的 Bcl-2 抑制劑,Ki 小于0.01 nM。Venetoclax 可以誘導(dǎo)自噬 (autophagy) 作用。


生物活性

Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy


體外研究(In Vitro)

Venetoclax (ABT-199) potently kills FL5.12-BCL-2 cells (EC50=4 nM), Venetoclax (ABT-199) shows much weaker activity against FL5.12-BCL-XL cells (EC50=261 nM). ABT-199 also shows selectivity in cellular mammalian two-hybrid assays, where it disrupts BCL-2-BIM complexes (EC50=3 nM) but is much less effective against BCL-XL-BCL-XS (EC50=2.2 μM) or MCL-1-NOXA complexes[


體內(nèi)研究(In Vivo)

After a single oral dose of 12.5 mg per kg body weight in xenografts derived from RS4;11 cells (ALL), Venetoclax (ABT-199) causes a maximal tumor growth inhibition (TGImax) of 47% (P<0.001) and tumor growth delay (TGD) of 26% (P<0.05)[1].
Treatment of established xenografted (a mouse xenograft model of the T-ALL cell line LOUCY) tumors with Venetoclax (ABT-199) 100 mg/kg for 4 days results in a significant reduction of leukemic burden


Clinical Trial

NCT NumberSponsorConditionStart DatePhase
NCT04282811Gruppo Italiano Malattie EMatologiche dell′Adulto
Chronic Lymphocytic Leukemia|Relapse Leukemia|Refractory Leukemia
July 24, 2020
NCT03112174Pharmacyclics LLC.|Janssen Research & Development, LLC
Mantle-Cell Lymphoma
May 12, 2017Phase 3
NCT03343678Boehringer Ingelheim
Leukemia, Lymphocytic, Chronic, B-Cell
January 17, 2018Phase 1



分子量:868.44


Formula:C45H50ClN7O7S


CAS 號(hào):1257044-40-8


中文名稱:維奈妥拉


運(yùn)輸條件:Room temperature in continental US; may vary elsewhere.


儲(chǔ)存方式:

Powder-20°C3 years

4°C2 years
In solvent-80°C6 months

-20°C1 month


溶解性數(shù)據(jù)


DMSO : 77.5 mg/mL (89.24 mM; Need ultrasonic)

Ethanol : < 1 mg/mL (insoluble)

配制儲(chǔ)備液
濃度溶劑體積質(zhì)量1 mg5 mg10 mg
1 mM1.1515 mL5.7575 mL11.5149 mL
5 mM0.2303 mL1.1515 mL2.3030 mL
10 mM0.1151 mL0.5757 mL1.1515 mL
*

請(qǐng)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(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 儲(chǔ)存時(shí),請(qǐng)?jiān)?6 個(gè)月內(nèi)使用,-20°C 儲(chǔ)存時(shí),請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。

In Vivo:

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

——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)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(qǐng)依序添加每種溶劑: 60% phosal 50 propylene glycol (PG), 30% polyethylene glycol 400 (PEG400), 10% ethanol

    Solubility: 20 mg/mL (23.03 mM); Suspended solution; Need ultrasonic


  • 2.


    請(qǐng)依序添加每種溶劑: 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 5.25 mg/mL (6.05 mM); Clear solution


  • 3.


    請(qǐng)依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.58 mg/mL (2.97 mM); Clear solution


  • 4.


    請(qǐng)依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (2.88 mM); Suspended solution; Need ultrasonic and warming


參考文獻(xiàn)

[1]. Souers AJ, et al. ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets. Nat Med. 2013 Feb;19(2):202-8.

[2]. Peirs S, et al. ABT-199 mediated inhibition of BCL-2 as a novel therapeutic strategy in T-cell acute lymphoblastic leukemia. Blood. 2014 Dec 11;124(25):3738-47.

[3]. Bi C, et al. Inhibition of 4EBP phosphorylation mediates the cytotoxic effect of mechanistic target of rapamycin kinase inhibitors in aggressive B-cell lymphomas. Haematologica. 2017 Apr;102(4):755-764.


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