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Venetoclax

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Chemical Structure| 1257044-40-8 同义名 : ABT-199;GDC-0199;RG 7601. Venetoclax.;RG7601
CAS号 : 1257044-40-8
货号 : A156386
分子式 : C45H50ClN7O7S
纯度 : 99%
分子量 : 868.439
MDL号 : MFCD23160052
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 80 mg/mL(92.12 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：

5% DMSO+50% PEG 300+5% Tween 80+water 5 mg/mL

生物活性
靶点

  • Bcl-2

    Bcl-2, Ki:<0.01 nM
描述 Bcl-2 (B-cell lymphoma 2) is the first identified apoptotic regulator. It belongs to Bcl-2 family commitment to PCD, which regulates apoptosis, pro-apoptosis or anti-apoptosis. ABT-199 is a highly potent inhibitor of Bcl-2, re-engineered from ABT-263. It has subnanomolar affinity (Ki<0.010 nM, analysis by TR–FRET assay), which is over three orders of magnitude to Bcl-XL (Ki=48nM) and Bcl-W (Ki=245 nM). ABT-199 can disrupt BCL-2–BIM complex and induce multiple hallmarks of apoptosis, including cytochrome c release, caspase activation, the externalization of phosphatidylserine and the accumulation of sub-G0/G1 DNA, with lower concentration than ABT-263. Thus it facilitates ABT-199 to have cell-killing activity to Bcl-2 high-expressed NHL cell lines. ABT-199 can inhibit tumor xenograft growth as a single agent or combination with rituximab and bendamustine.[1]
作用机制 ABT-199 is complicated by the high degree of similarity within the BH3-binding domains of Bcl-2 and Bcl-XL.[1]
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
ALL-SIL 10 μM Growth Inhibition Assay 48 h IC50=0.1803 μM 25301704
CCRF-CEM 10 μM Growth Inhibition Assay 48 h IC50=1.360 μM 24342948
CS-THL1 20 nM Growth Inhibition Assay 72 h Inhibits cell growth assessed by cell viability 25916698
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
NCT03342144 - Recruiting December 31, 2020 Germany ... 展开 >> Onkologische Praxis /ID# 201545 Recruiting Stuttgart, Baden-Wuerttemberg, Germany, 70174 Medizinisches Versorgungszentrum (MVZ) /ID# 201548 Recruiting Aschaffenburg, Bayern, Germany, 63739 Studienzentrum Aschaffenburg /ID# 204125 Recruiting Aschaffenburg, Bayern, Germany, 63739 Praxis Dres. Hornberger & Kollegen /ID# 202613 Recruiting Bad Reichenhall, Bayern, Germany, 83435 Onkologie am Segelfliegerdamm /ID# 202603 Recruiting Berlin, Bayern, Germany, 12487 Onkologie Hof /ID# 201531 Recruiting Hof, Bayern, Germany, 95028 Praxis Dr. Vehling-Kaiser /ID# 202614 Recruiting Landshut, Bayern, Germany, 84028 Praxis Dres. Grüner/Hejazi/Niewenhuys /ID# 202602 Recruiting Weiden i.d.OPf., Bayern, Germany, 92637 Praxis Dr. Kreher /ID# 202604 Recruiting Bad Liebenwerda, Brandenburg, Germany, 04924 MVZ Dres. Cordes & Partner /ID# 202598 Recruiting Frankfurt am Main, Hessen, Germany, 60596 OAZ Hannover /ID# 201538 Recruiting Hanover, Niedersachsen, Germany, 30171 Onkolologische Praxis Oldenburg /ID# 202607 Recruiting Oldenburg, Niedersachsen, Germany, 26121 MVZ der Paracelsus-Klinik /ID# 201541 Recruiting Osnabrück, Niedersachsen, Germany, 49076 Med. Studiengesellschaft Nord West GmbH /ID# 201535 Recruiting Westerstede, Niedersachsen, Germany, 26655 Onkozentrum Dresden /ID# 202599 Recruiting Dresden, Sachsen, Germany, 01127 BAG Freiberg-Richter /ID# 201532 Recruiting Dresden, Sachsen, Germany, 01307 Onkologische Schwerpunktpraxis /ID# 200953 Recruiting Berlin, Germany, 10707 Internistische Schwerpunktprax /ID# 200949 Recruiting Erlangen, Germany, 91052 Luebecker Oncology Practice /ID# 200952 Recruiting Luebeck, Germany, 23562 Stauferklinikum Schwaebisch Gm /ID# 201518 Recruiting Mutlangen, Germany, 73557 收起 <<
NCT03112174 Mantle-Cell Lymphoma Phase 3 Recruiting September 2022 -
NCT03672695 Acute Myeloid Leukaemia Phase 1 Not yet recruiting March 31, 2022 United States, Connecticut ... 展开 >> Smilow Cancer Hospital at Yale Not yet recruiting New Haven, Connecticut, United States, 06511 United States, Texas The University of Texas MD Anderson Cancer Center, Houston, TX Not yet recruiting Houston, Texas, United States, 77030 Australia Peter MacCallum cancer centrer Not yet recruiting Melbourne, Australia The Alfred Hospital Department of Haematology Not yet recruiting Victoria Park, Australia France Institut Paoli-Calmettes Not yet recruiting Marseille, France Hopital Saint-Antoine Not yet recruiting Paris, France Institut Universitaire du Cancer Toulouse - Oncopole Not yet recruiting Toulouse, France 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.15mL

0.23mL

0.12mL

5.76mL

1.15mL

0.58mL

11.51mL

2.30mL

1.15mL
参考文献

[1]Souers AJ, Leverson JD, 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]Choo EF, Boggs J, et al. The role of lymphatic transport on the systemic bioavailability of the Bcl-2 protein family inhibitors navitoclax (ABT-263) and ABT-199. Drug Metab Dispos. 2014 Feb;42(2):207-12.

[3]Punnoose EA, Leverson JD, et al. Expression Profile of BCL-2, BCL-XL, and MCL-1 Predicts Pharmacological Response to the BCL-2 Selective Antagonist Venetoclax in Multiple Myeloma Models. Mol Cancer Ther. 2016 May;15(5):1132-44.