Venetoclax (ABT-199, GDC-0199)

目录号:S8048

Venetoclax (ABT-199, GDC-0199) Chemical Structure

Molecular Weight(MW): 868.44

Venetoclax (ABT-199, GDC-0199)是一种Bcl-2选择性抑制剂,无细胞试验中Ki为<0.01 nM,比作用于Bcl-xL和Bcl-w选择性高4800倍以上,对Mcl-1没有抑制活性。Phase 3。

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客户使用该产品的3个实验数据:

  • THP-1 cells were treated with cytarabine alone and in combination with ABT-199 for 8 h. Whole cell lysates were extracted and subjected to Western blotting, and probed with anti-γH2AX or -β-actin antibody. Densitometry for γH2AX expression was measured, normalized to β-actin, and graphed as fold change compared to the no drug control. The data are presented as mean ± standard error from at least 3 independent Western blots. * indicates p < 0.05.

    Mol Oncol 2014 10.1016/j.molonc.2014.09.008. Venetoclax (ABT-199, GDC-0199) purchased from Selleck.

    C33A cells were treated with ABC294640 (5 μmol/L), together with/out ABT-737 (200 nM) or GDC-0199 (200 nM), cells were further cultured for indicated time, cell growth (MTT assay, (A) and apoptosis (Histone DNA ELISA assay, (B) were tested.

    Oncotarget, 2017, 9(2):2384-2394. Venetoclax (ABT-199, GDC-0199) purchased from Selleck.

  • CLL cells were incubated with drugs immediately or co-cultured on CD154 stroma overnight and incubated with the indicated concentrations of ABT-199.

    J Biol Chem 2014 289(23), 16190-9. Venetoclax (ABT-199, GDC-0199) purchased from Selleck.

产品安全说明书

Bcl-2抑制剂选择性比较

生物活性

产品描述 Venetoclax (ABT-199, GDC-0199)是一种Bcl-2选择性抑制剂,无细胞试验中Ki为<0.01 nM,比作用于Bcl-xL和Bcl-w选择性高4800倍以上,对Mcl-1没有抑制活性。Phase 3。
特性 ABT-263 (Navitoclax)的重组
靶点
Bcl-2 [1]
(Cell-free assay)
<0.01 nM(Ki)
体外研究

ABT-199 对Bcl-xL, Mcl-1 和Bcl-w具有低的敏感性,Ki分别为48 nM, >444 nM 和 245 nM。ABT-199 有效抑制FL5.12-Bcl-2 细胞, RS4;11细胞, EC50分别为4 nM 和 8 nM,作用于 FL5.12-Bcl-xL细胞具有低活性,EC50为261 nM。ABT-199 诱导RS4;11 细胞快速凋亡,细胞色素c释放,caspase激活,磷脂酰丝氨酸外化,及sub-G0/G1 DNA积累。定量免疫印迹表明,ABT-199对包括NHL,DLBCL,MCL,AML和ALL细胞系的灵敏度,与Bcl-2的表达强烈相关。ABT-199也诱导 CLL 凋亡,平均EC50 为3.0 nM。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CS-THL1 NEHx[ZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHLOWtVOjBibl2= MluzO|IhcA>? MoHPSG1UVw>? Mk\HTY5pcWKrdIOgZ4VtdCCpcn;3eIgh[XO|ZYPz[YQh[nliY3XscEB3cWGkaXzpeJk> NUDNcYNjOjV7MU[2PVg>
CS-THL1 M173eWFxd3C2b4TpZ{BCe3OjeR?= MUiyOUBvVQ>? MUTEUXNQ NFPwTFRKdmS3Y3XzJIFxd3C2b4Ppdy=> M4KyWlI2QTF4Nkm4
DoGKiT NHLlSW1CeG:ydH;0bYMhSXO|YYm= M1fzN|UxKG6P MnvzSG1UVw>? M1S4VGlv\HWlZYOgZZBweHSxc3nz Ml7DNlU6OTZ4OUi=
RS4-11 NYPaOGhDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;6N4NTPzJiaB?= MlXXTWM2OD1yLkC0NFIh|ryP Ml3zNlU3PDl5Nki=
NALM-6 M{LnbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLQO|FxPzJiaB?= MYTJR|UxRjNizszN NI\5W24zPTZ2OUe2PC=>
SU-DHL-6 M3XFOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXkNE45KM7:TR?= M2O0Z2lvcGmkaYTzJINmdGxiZ4Lve5RpKGG|c3Xzd4VlKGK7IHPlcIwhfmmjYnnsbZR6 MYiyOVU6ODhyMx?=
OCI-Ly19 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV[xJO69VQ>? M2\oZ2lvcGmkaYTzJINmdGxiZ4Lve5RpKGG|c3Xzd4VlKGK7IHPlcIwhfmmjYnnsbZR6 MnzLNlU2QTB6MEO=
SU-DHL-6 MWPGeY5kfGmxbjDBd5NigQ>? MXiwMlc2KM7:TR?= Mm\qNVghcA>? NEOwc5hKdmO{ZXHz[ZMheHKxLYP1dpZqfmGuIIDyc5RmcW5iTVPMMVEh\XiycnXzd4lwdg>? NYWzO5hGOjV3OUC4NFM>
KCL22 MUfGeY5kfGmxbjDBd5NigQ>? Ml7CNkDPxE1? NF;3UpI1QCCq NH[5WmhFVVOR MXTJcoNz\WG|ZYOgSG5CKG[{YXfhcYVvfGG2aX;u NF3KUVMzPTN|M{K1Ni=>
LOUCY MnvuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFixfXcyOCEQvF2= M{HsU|Q5KGh? NXXYcmZMTE2VTx?= NUHCenVPUUN3ME2wMlAyOzlizszN M{DoTVI2OzBzN{C0
ALL-SIL Mm[0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fIeFExKM7:TR?= NEexdoE1QCCq MWjEUXNQ MlTITWM2OD1yLkG4NFMh|ryP MXmyOVMxOTdyNB?=
CUTLL1 MlG2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XSO|ExKM7:TR?= MnLIOFghcA>? MX;EUXNQ NFLyepBKSzVyPUCuN|gzOyEQvF2= MYKyOVMxOTdyNB?=
KOPTK1 NWmwTmlPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV[xNEDPxE1? MYW0PEBp MkjaSG1UVw>? NXPGbW1UUUN3ME2wMlY1OzJizszN MYSyOVMxOTdyNB?=
DND-41 NVvPTJFUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fCc|ExKM7:TR?= MkfiOFghcA>? M1O0PWROW09? M4PWbmlEPTB;MT65Olk2KM7:TR?= MlvWNlU{ODF5MES=
PF-382 NGXteIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXSxNEDPxE1? M1jwUFQ5KGh? NHW5cYRFVVOR NULkZopQUUN3ME2yMlE5OjRizszN NFz1dXczPTNyMUewOC=>
KARPAS-45 MmDyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mkj0NVAh|ryP MofHOFghcA>? NGG5W2VFVVOR NHPTfm5KSzVyPUOuNlIzPSEQvF2= NHfKe3MzPTNyMUewOC=>
PEER NGrqcJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1r5OVExKM7:TR?= MUS0PEBp MWXEUXNQ M4nwUmlEPTB;ND62OFA{KM7:TR?= NFXxOG0zPTNyMUewOC=>
CX-1 NF72ZVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnRNZZSOTByIN88US=> MoHFO|IhcA>? MknuTWM2OD14Lkeg{txO MlTQNlUzODh6OEK=
LS147T MlfUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn2zNVAxKM7:TR?= MXG3NkBp M1XUSWlEPTB;MkmuOUDPxE1? MkHXNlUzODh6OEK=
HL-60 M125ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYe0PEBp MkXzTWM2ODxzIN88US=> MljnNlQ{PDZzMU[=
MOLM-13 NGTHOGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HkfFQ5KGh? M2TifmlEPTB:MTFOwG0> NIW0XWMzPDN2NkGxOi=>
OCI-AML2 MkXDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXW0PEBp M3izTGlEPTB:MTFOwG0> NGHCNmMzPDN2NkGxOi=>
Kasumi-1 NWPKdokyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfBSWFpPDhiaB?= NX;xXY5mUUN3MEyxJO69VQ>? NEXEPWQzPDN2NkGxOi=>
KG-1 M1HzWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLlOFghcA>? M4rsW2lEPTB:MTFOwG0> MX:yOFM1PjFzNh?=
THP-1 NHOxe|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWS0PEBp NU\VRmJYUUN3MEyxJO69VQ>? NVXOUVFsOjR|NE[xNVY>
MOLM-14 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLUOFghcA>? M3PlZ2lEPTB:MTFOwG0> M1jMc|I1OzR4MUG2
MOLM-13 MojiRZBweHSxdHnjJGF{e2G7 NUmxdZR1PTBibl2= MXeyOEBp MW\BdI9xfG:|aYOgbY5lfWO2aX;u M1j3cFI1OzR4MUG2
HSB NVPxUHEzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWSxNEDPxE1? M4LjcFQ5KGh? MkC1SG1UVw>? NH;rfmhKSzVyPUSuOFQ5KM7:TR?= NXiySnd3OjR|NEK5OFg>
MOLT4 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rBdlExKM7:TR?= M3;RelQ5KGh? NE\zd45FVVOR M375OGlEPTB;ND6xOVQh|ryP NWf5cFE4OjR|NEK5OFg>
SKW-3/KE-37 NVy5RmFMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEX0U|cyOCEQvF2= MUO0PEBp MonMSG1UVw>? NWK4OXN[UUN3ME2wMlcyOiEQvF2= MnvGNlQ{PDJ7NEi=
SUPT-11 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rQ[FExKM7:TR?= NIfXSVE1QCCq M17wTWROW09? NHH0TWVKSzVyPUSuOFc{KM7:TR?= M{HYe|I1OzR{OUS4
JURKAT NEXjZlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWixNEDPxE1? NIn0Rno1QCCq MlLtSG1UVw>? MXHJR|UxRTRwOEmzJO69VQ>? MWSyOFM1Ojl2OB?=
CCRF-CEM MlPVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfDepgyOCEQvF2= MnvkOFghcA>? M3LxS2ROW09? MYDJR|UxRTFwM{[wJO69VQ>? M2DiUlI1OzR{OUS4
LOUCY MWrBdI9xfG:2aXOgRZN{[Xl? NWrT[|l{OiEQvF2= MXy0PEBp MmiwSG1UVw>? MWnBdI9xfG:|aYOgbY5lfWO2aX;u M1vSOFI1OzR{OUS4

... Click to View More Cell Line Experimental Data

体内研究 ABT-199 (100 mg/kg)处理RS4;11 移植瘤,产生的最大肿瘤生长抑制率为95%,肿瘤生长延迟152%。ABT-199单独处理或与SDX-105及其他药剂联用处理DoHH2和Granta-519移植瘤,也抑制肿瘤生长。[1]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
+ 展开

亲和力分析:

竞争性荧光偏振检测测定ABT-199对Bcl-2家族的不同亚型的亲和力(Ki 或 IC50)。使用如下肽探针/蛋白对:f-bad (1 nM) 与Bcl-xL (6 nM), f-Bax (1 nM) 与 Bcl-2 (10 nM),f-Bax(1 nM) 与Bcl-w (40 nM), f-Noxa(2 nM) 与Mcl-1 (40 nM), 及 f-Bax (1 nM)与Bcl-2-A1(15 nM)。使用时间分辨荧光共振能量转移检测测定对Bcl-xL的亲和力。Bcl-xL (1 nM, His标记的 ) 与200 nM f-Bak, 1 nM Tb标记的anti-His抗体, 及 ABT-199,在室温下混合30分钟。在Envision酶标仪上,使用340/35 nm 激发滤光片及520/525 (f-Bak) 和495/510 nm (Tb标记的anti-His抗体) 发射滤光片,测量荧光值。
细胞实验:[1]
+ 展开
  • Cell lines: NHL, DLBCL, MCL, AML 和 ALL 细胞系
  • Concentrations: ~1 μM
  • Incubation Time: 48 小时
  • Method: RS4;11 细胞按每孔5×104个接种在96孔板中,使用初始1 μM-0.05 nM。在半对数期稀释的ABT-199 处理细胞。白血病和淋巴瘤细胞系按每孔1.5-2×104个接种在合适的培养基中,与ABT-199温育48小时。使用Cell TiterGlo 试剂测定对细胞增殖的影响。通过对浓度-反应数据非线性回归分析测定EC50值。
    (Only for Reference)
动物实验:[1]
+ 展开
  • Animal Models: 雌性 C.B-17 SCID 小鼠(携带DoHH2 和Granta-519 移植瘤) 和雌性 C.B-17 SCID-beige 小鼠 (携带RS4;11和 Toledo 移植瘤)
  • Formulation: 60% Phosal 50丙二醇(PG), 30%聚乙二醇(PEG) 400 和 10% 乙醇
  • Dosages: ~100 mg/kg
  • Administration: 口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL warmed (115.14 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
5% DMSO+50% PEG 300+5% Tween 80+ddH2O
5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 868.44
化学式

C45H50ClN7O7S

CAS号 1257044-40-8
稳定性 powder
in solvent
别名 N/A

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02756897 Recruiting Leukemia|Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma M.D. Anderson Cancer Center|AbbVie July 7, 2016 Phase 2
NCT03036904 Not yet recruiting Diffuse Large B-Cell Lymphoma|High Grade B-Cell Lymphoma Weill Medical College of Cornell University|Genentech, Inc.|Massachusetts General Hospital|M.D. Anderson Cancer Center February 6, 2017 Phase 1
NCT02951117 Not yet recruiting Multiple Myeloma AbbVie May 2017 Phase 1
NCT02966756 Not yet recruiting Chronic Lymphocytic Leukemia (CLL) AbbVie|Genentech/Roche April 2017 Phase 2
NCT02966782 Not yet recruiting Myelodysplastic Syndromes (MDS) AbbVie|Genentech, Inc. March 2017 Phase 1
NCT03045328 Not yet recruiting Recurrent Chronic Lymphocytic Leukemia|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Refractory Small Lymphocytic Lymphoma Steven E. Coutre|Stanford University March 2017 Phase 1|Phase 2

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操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    Could you please offer some advice on the half-life of the drug ?

  • 回答:

    According to the reference (https://www.ncbi.nlm.nih.gov/pubmed/24212376), the half-life of ABT-199 in dogs is 12.9 hr.

  • 问题 2:

    how to prepare the working solution for mice including how to dissolve the powder?

  • 回答:

    We recommend the following vehicle for ABT 199, 30% PEG400/0.5% Tween80/5% Propylene glycol (64.5% water, V/V), at a concentration up to 20mg/ml. Its a homogeneous suspension and can be used for oral gavage.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID