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5个实验数据:

  • (b) MV4-11 cells were treated in vitro with ABT-199 (0.01, 0.1, 1 or 10 μM) with or without BL-8040 (20 μM) for 24 h in 1% FCS RPMI medium. The percentage of dead cells (PI+ cells) was evaluated by FACS. (c) miR-15a and miR-16-1 transfections were performed using Lipofectamine 2000 transfection reagent. At 72 h post-transfection, cells were stained with Annexin-V and PI. FACS plots and numerical data of % cells are shown. The results are expressed as the mean±s.d. and were analyzed using Student’s t-test (*P ⩽0.05 compared with control).

    Leukemia, 2017, 31(11):2336-2346. Venetoclax (ABT-199, GDC-0199) purchased from Selleck.

    MDA-MB-468 cells were treated with BETd-246 (50 nM), BM-1197 (250 nM), ABT-263 (250 nM), ABT-199 (250 nM) or A-1155463 (250 nM) as indicated for 24 h for Annexin V-PI apoptosis analysis. Data are the mean ± SEM (n=3).

    Cancer Res, 2017, 77(9):2476-2487. Venetoclax (ABT-199, GDC-0199) purchased from Selleck.

  • 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 MoD4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWSyNEBvVQ>? MkTqO|IhcA>? M2W5NmROW09? M1XPWWlvcGmkaYTzJINmdGxiZ4Lve5RpKGG|c3Xzd4VlKGK7IHPlcIwhfmmjYnnsbZR6 MYiyOVkyPjZ7OB?=
CS-THL1 M4jMWGFxd3C2b4TpZ{BCe3OjeR?= MoS1NlUhdk1? MlLXSG1UVw>? M17yeGlv\HWlZYOgZZBweHSxc3nz M4TQclI2QTF4Nkm4
DoGKiT MV;BdI9xfG:2aXOgRZN{[Xl? NVX6e5E2PTBibl2= MV;EUXNQ Mne5TY5lfWOnczDhdI9xfG:|aYO= NX:yZVF2OjV7MU[2PVg>
RS4-11 M3vaXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3ZO|IhcA>? NHnvRY9KSzVyPUCuNFQxOiEQvF2= NFvkXFMzPTZ2OUe2PC=>
NALM-6 M1r1N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorIO|IhcA>? NUnsXFc1UUN3ME6zJO69VQ>? MlW3NlU3PDl5Nki=
SU-DHL-6 M1O2W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIm2eGkxNjhizszN M2jvbWlvcGmkaYTzJINmdGxiZ4Lve5RpKGG|c3Xzd4VlKGK7IHPlcIwhfmmjYnnsbZR6 M2fxeVI2PTlyOECz
OCI-Ly19 Ml\wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\5NUDPxE1? NGO4XIpKdmirYnn0d{Bk\WyuIHfyc5d1cCCjc4Pld5Nm\CCkeTDj[YxtKH[rYXLpcIl1gQ>? NW\NRYl6OjV3OUC4NFM>
SU-DHL-6 MYjGeY5kfGmxbjDBd5NigQ>? M2P3W|AvPzVizszN M{PrPVE5KGh? MnLQTY5kemWjc3XzJJBzdy2|dYL2bZZidCCycn;0[YlvKE2FTD2xJIV5eHKnc4Ppc44> M{LTXVI2PTlyOECz
KCL22 MoSzSpVv[3Srb36gRZN{[Xl? NEm1TpozKM7:TR?= MmLaOFghcA>? MoDOSG1UVw>? NGH5cVVKdmO{ZXHz[ZMhTE6DIH\yZYdidWWwdHH0bY9v MVOyOVM{OzJ3Mh?=
LOUCY NEe0c3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYiwVXdpOTBizszN MoTVOFghcA>? M37NUGROW09? NF;VU|JKSzVyPUCuNFE{QSEQvF2= NU\hZpJMOjV|MEG3NFQ>
ALL-SIL M4\Cdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnFNXkxOTBizszN MU[0PEBp NVHiOJFYTE2VTx?= NEHEVFJKSzVyPUCuNVgxOyEQvF2= NHHrVYQzPTNyMUewOC=>
CUTLL1 Ml[1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVixPXYyOTBizszN MoLxOFghcA>? MYHEUXNQ NIXneldKSzVyPUCuN|gzOyEQvF2= MYiyOVMxOTdyNB?=
KOPTK1 MnjZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjnTlUyOCEQvF2= M1S1SVQ5KGh? Mn3CSG1UVw>? NGqzRYxKSzVyPUCuOlQ{OiEQvF2= NHfYV44zPTNyMUewOC=>
DND-41 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHiZ5QyOCEQvF2= M{n0O|Q5KGh? NV6zNG14TE2VTx?= NYPzUoVpUUN3ME2xMlk3QTVizszN NXXFSHJXOjV|MEG3NFQ>
PF-382 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDwc3YyOCEQvF2= NIHhU2o1QCCq M2TmZmROW09? MnzkTWM2OD1{LkG4NlQh|ryP MVWyOVMxOTdyNB?=
KARPAS-45 MoHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzWd|kyOCEQvF2= NUPI[Io5PDhiaB?= MXLEUXNQ NXu4O4xWUUN3ME2zMlIzOjVizszN M1\jSlI2OzBzN{C0
PEER NXq5fVRvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXuxNEDPxE1? M1XuVlQ5KGh? M3nyb2ROW09? M4\tPWlEPTB;ND62OFA{KM7:TR?= MoD0NlU{ODF5MES=
CX-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3[4UFExOCEQvF2= MXm3NkBp NVvpSI1iUUN3ME22Mlch|ryP MnXVNlUzODh6OEK=
LS147T M2PZU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rnUVExOCEQvF2= M3;Tb|czKGh? MYLJR|UxRTJ7LkWg{txO M2TYW|I2OjB6OEiy
HL-60 M{nrWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\pc5BEPDhiaB?= MY\JR|UxRDFizszN NWPOVWNFOjR|NE[xNVY>
MOLM-13 NFfHV|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV:0PEBp NW[1ZoFmUUN3MEyxJO69VQ>? NIfwVlYzPDN2NkGxOi=>
OCI-AML2 NXPCVG15T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfKe4tYPDhiaB?= Mo[3TWM2ODxzIN88US=> NH74dHczPDN2NkGxOi=>
Kasumi-1 NVXZNIN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLQOFghcA>? NX65bnFUUUN3MEyxJO69VQ>? NFPNXIMzPDN2NkGxOi=>
KG-1 NXvGfok2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;WW3Z4PDhiaB?= MV;JR|UxRDFizszN M2D6RlI1OzR4MUG2
THP-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jXXVQ5KGh? M2fQdGlEPTB:MTFOwG0> NFPJRWwzPDN2NkGxOi=>
MOLM-14 NIDacXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;2OFghcA>? M3fXT2lEPTB:MTFOwG0> M3foWVI1OzR4MUG2
MOLM-13 M3nlSGFxd3C2b4TpZ{BCe3OjeR?= MoHqOVAhdk1? NH\VdFMzPCCq NIT4d|JCeG:ydH;zbZMhcW6mdXP0bY9v Mn63NlQ{PDZzMU[=
HSB NI\NOYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3riXVExKM7:TR?= NE\xNXE1QCCq NHLjXmNFVVOR Mo\0TWM2OD12LkS0PEDPxE1? NHzUWXYzPDN2Mkm0PC=>
MOLT4 MlS0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;6VoxrOTBizszN MX:0PEBp M3rNe2ROW09? NUj6SXVTUUN3ME20MlE2PCEQvF2= NHLuVZUzPDN2Mkm0PC=>
SKW-3/KE-37 M{S3Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\6VogyOCEQvF2= NV;3cVFQPDhiaB?= MlnQSG1UVw>? MVzJR|UxRTBwN{GyJO69VQ>? NUP5O3RlOjR|NEK5OFg>
SUPT-11 MlX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoT4NVAh|ryP Ml:4OFghcA>? MkfrSG1UVw>? NGOwWHdKSzVyPUSuOFc{KM7:TR?= M4L1TVI1OzR{OUS4
JURKAT MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLSSI12OTBizszN NHvRSo01QCCq MmfGSG1UVw>? M3f6bmlEPTB;ND64PVMh|ryP NFnaXYIzPDN2Mkm0PC=>
CCRF-CEM MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVixNEDPxE1? MmTIOFghcA>? MVXEUXNQ NWLsfmE{UUN3ME2xMlM3OCEQvF2= NIDuN5czPDN2Mkm0PC=>
LOUCY Ml;GRZBweHSxdHnjJGF{e2G7 M3TpbVIh|ryP M1XXeVQ5KGh? MYXEUXNQ MYLBdI9xfG:|aYOgbY5lfWO2aX;u NV7OZZRmOjR|NEK5OFg>

... 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
NCT03735875 Not yet recruiting Acute Myeloid Leukemia With FLT3/ITD Mutation|FLT3 Gene Mutation|FLT3 Internal Tandem Duplication|Recurrent Acute Myeloid Leukemia|Refractory Acute Leukemia M.D. Anderson Cancer Center|National Cancer Institute (NCI) March 31 2019 Phase 1|Phase 2
NCT03708003 Not yet recruiting Relapsed/Refractory Chronic Lymphocytic Leukemia|Chronic Lymphocytic Leukemia|Leukemia Swiss Group for Clinical Cancer Research March 2019 Phase 2
NCT03710772 Not yet recruiting CD20 Positive|Mantle Cell Lymphoma M.D. Anderson Cancer Center|National Cancer Institute (NCI) January 31 2019 Phase 2
NCT03701321 Not yet recruiting Recurrent Plasma Cell Myeloma|Refractory Plasma Cell Myeloma National Cancer Institute (NCI) January 25 2019 Phase 1|Phase 2
NCT03639324 Not yet recruiting Chronic Lymphocytic Leukemia|CLL|Relapsed CLL|Refractory Chronic Lymphocytic Leukemia|Relapsed Chronic Lymphocytic Leukemia Virginia Commonwealth University January 31 2019 Phase 1
NCT03573024 Not yet recruiting Acute Myeloid Leukemia University of Colorado Denver January 2019 Phase 2

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

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