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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。
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 Number | Sponsor | Condition | Start Date | Phase |
---|---|---|---|---|
NCT04282811 | Gruppo Italiano Malattie EMatologiche dell′Adulto | July 24, 2020 | ||
NCT03112174 | Pharmacyclics LLC.|Janssen Research & Development, LLC | May 12, 2017 | Phase 3 | |
NCT03343678 | Boehringer Ingelheim | January 17, 2018 | Phase 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°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
溶解性數(shù)據(jù)
DMSO : 77.5 mg/mL (89.24 mM; Need ultrasonic)
Ethanol : < 1 mg/mL (insoluble)
濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
---|
1 mM | 1.1515 mL | 5.7575 mL | 11.5149 mL |
5 mM | 0.2303 mL | 1.1515 mL | 2.3030 mL |
10 mM | 0.1151 mL | 0.5757 mL | 1.1515 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。
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
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
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)
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 Number | Sponsor | Condition | Start Date | Phase |
---|---|---|---|---|
NCT04282811 | Gruppo Italiano Malattie EMatologiche dell′Adulto | July 24, 2020 | ||
NCT03112174 | Pharmacyclics LLC.|Janssen Research & Development, LLC | May 12, 2017 | Phase 3 | |
NCT03343678 | Boehringer Ingelheim | January 17, 2018 | Phase 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°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
溶解性數(shù)據(jù)
DMSO : 77.5 mg/mL (89.24 mM; Need ultrasonic)
Ethanol : < 1 mg/mL (insoluble)
濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
---|
1 mM | 1.1515 mL | 5.7575 mL | 11.5149 mL |
5 mM | 0.2303 mL | 1.1515 mL | 2.3030 mL |
10 mM | 0.1151 mL | 0.5757 mL | 1.1515 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。
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
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
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)