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ABT-199 (GDC-0199),Bcl-2抑制剂

高效的选择性Bcl-2抑制剂。
规格或纯度: ≥99%
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货号 (SKU) 包装规格 是否现货 价格 数量
A124869-5mg
 5mg 现货 Stock Image
A124869-10mg
 10mg 现货 Stock Image
A124869-25mg
 25mg 现货 Stock Image
A124869-50mg
 50mg 现货 Stock Image
A124869-100mg
 100mg 现货 Stock Image
A124869-500mg
 500mg 现货 Stock Image
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Bcl-2-like 1 Antagonist Bcl-2-like 2 Antagonist BCL2 apoptosis regulator Antagonist MCL1 apoptosis regulator，BCL2 family member Antagonist
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基本描述

规格或纯度 ≥99%
英文名称 ABT-199 (GDC-0199)
别名 GDC-0199|维奈妥拉|4-(4-｛[2-(4-氯苯基)-4,4-二甲基环己-1-烯-1-基]甲基｝哌嗪-1-基)-N-(｛3-硝基-4-[(四氢-2H-吡喃-4-基甲基)氨基]苯基｝磺酰基)-2-(1H-吡咯并[2,3-b]吡啶-5-基氧基)苯甲酰胺)
英文别名 Venetoclax|1257044-40-8|ABT-199|Venclexta|GDC-0199|ABT199|ABT 199|venclyxto|RG7601|UNII-N54AIC43PW|GDC 0199|RG-7601|Venetoclax (ABT199)|N54AIC43PW|Venetoclax; Abt-199|Venetoclax(ABT-199)|4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperaz
生化机理 ABT-199 is a potent and selective inhibitor of B-cell lymphoma-2 (BCL-2) family proteins, currently in clinical trials. ABT-199 inhibits the growth of BCL-2-dependent tumors in vivo and spares human platelets. A single dose of ABT-199 in three patients with refractory chronic lymphocytic leukemia resulted in tumor lysis within 24 h. These data indicate that selective pharmacological inhibition of BCL-2 shows promise for the treatment of BCL-2-dependent hematological cancers.Potent, selective Bcl-2 inhibitor (K i <0.01 nM) that inhibits the growth of Bcl-2–dependent tumors while sparing platelets. Bcl-2–specific BH3 mimetic. Promising agent in the treatment\xa0of chronic lymphocytic leukaemic and estrogen receptor-positive br
储存温度 避光,-20°C储存
运输条件 超低温冰袋运输
产品介绍

ABT-199 (GDC-0199)是高效的Bcl-2选择性抑制剂，Ki为0.01 nM，比对Bcl-xL和Bcl-w的抑制性高4800倍以上，对Mcl-1无活性。A Bcl-2-selective inhibitor with Ki of <0.01 nM

ABT-199 (GDC-0199) is a BH3 mimetic that Bcl-2-selective inhibitor with Ki of <0.01 nM. B-cell lymphoma/leukemia 2 (Bcl-2) is an anti-apoptotic protein that controls cell survival by binding the BH3 domains of pro-death BAD and BAK proteins and preventing permeabilization of the mitochondrial outer membrane. This protein is tightly regulated for the homeostasis between cell growth and cell death.
A Bcl-2-selective inhibitor with Ki of <0.01 nM

名称和标识符

IUPAC Name 4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-N-[3-nitro-4-(oxan-4-ylmethylamino)phenyl]sulfonyl-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide
INCHI InChI=1S/C45H50ClN7O7S/c1-45(2)15-11-33(39(26-45)31-3-5-34(46)6-4-31)29-51-17-19-52(20-18-51)35-7-9-38(42(24-35)60-36-23-32-12-16-47-43(32)49-28-36)44(54)50-61(57,58)37-8-10-40(41(25-37)53(55)56)48-27-30-13-21-59-22-14-30/h3-10,12,16,23-25,28,30,48H,11,13-15,17-22,26-27,29H2,1-2H3,(H,47,49)(H,50,54)
InChi Key LQBVNQSMGBZMKD-UHFFFAOYSA-N
Canonical SMILES CC1(CCC(=C(C1)C2=CC=C(C=C2)Cl)CN3CCN(CC3)C4=CC(=C(C=C4)C(=O)NS(=O)(=O)C5=CC(=C(C=C5)NCC6CCOCC6)[N+](=O)[O-])OC7=CN=C8C(=C7)C=CN8)C
PubChem CID 49846579
分子量 868.44

化学和物理性质

溶解性 Soluble in DMSO (100 mg/ml (~115mM) at 25 °C), water (<1 mg/ml (< 1mM) at 25 °C), and ethanol (<1 mg/ml (< 1mM) at 25 °C).
敏感性 对光敏感
折光率 1.64

安全和危险性（GHS）

象形图
ghs08

Health Hazard

ghs07

Harmful
信号词 Danger
危险声明 H315: Causes skin irritation
H319: Causes serious eye irritation
H335: May cause respiratory irritation
H302: Harmful if swallowed
H372: Causes damage to organs through prolonged or repeated exposure
H361: Suspected of damaging fertility or the unborn child
预防措施声明 P261,P305+P351+P338,P280,P302+P352,P321,P405,P501,P264,P260,P271,P270,P304+P340,P403+P233,P362+P364,P330,P203,P264+P265,P301+P317,P318,P337+P317,P332+P317,P319

关联配体

Ligand ID 8318
名称 venetoclax
别名 GDC-0199
类别 Synthetic organic
学名 4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-N-[3-nitro-4-(oxan-4-ylmethylamino)phenyl]sulfonyl-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide
生物活性评价 Venetoclax is reported to be >4800-fold more selective for Bcl-2 compared to other protein family members Bcl-xL and Bcl-w .
评价 Venetoclax is a BH3 mimetic that selectively targets Bcl-2 , utilised for its pro-apoptotic activity. It is noteworthy that venetoclax is the first approved medicine designed to induce a natural process that helps cells self-destruct.
The IUPAC name provided by PubChem matches 'Example 5' claimed in patent US8580794 .
临床描述 The purpose of this open-label, multicenter, randomized, Phase III study is to evaluate the benefit of venetoclax in combination with rituximab compared with bendamustine in combination with rituximab in participants with relapsed or refractory CLL. Participants will be randomly assigned in 1:1 ratio to receive either venetoclax + rituximab (Arm A) or bendamustine + rituximab (Arm B).
This open-label, multicenter, randomized Phase III study is designed to compare the efficacy and safety of a combined regimen of obinutuzumab and venetoclax versus obinutuzumab + chlorambucil in participants with chronic lymphocytic leukemia (CLL) and coexisting medical conditions. The anticipated time on study treatment will be approximately one year and the follow-up period will be up to 5 years.
来源公司 Hoffmann-La Roche
Hoffmann-La Roche

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参考文献

1. Souers AJ, Leverson JD, Boghaert ER, Ackler SL, Catron ND, Chen J, Dayton BD, Ding H, Enschede SH, Fairbrother WJ et al..  (2013)  ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets..  Nat Med,  19  (2):  (202-8).  [PMID:23291630]
2. Tian BP, Xia LX, Bao ZQ, Zhang H, Xu ZW, Mao YY, Cao C, Che LQ, Liu JK, Li W et al..  (2017)  Bcl-2 inhibitors reduce steroid-insensitive airway inflammation..  J Allergy Clin Immunol,  140  (2):  (418-430).  [PMID:28043871]
3. Seymour JF, Kipps TJ, Eichhorst B, Hillmen P, D'Rozario J, Assouline S, Owen C, Gerecitano J, Robak T, De la Serna J et al..  (2018)  Venetoclax-Rituximab in Relapsed or Refractory Chronic Lymphocytic Leukemia..  N Engl J Med,  378  (12):  (1107-1120).  [PMID:29562156]
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