Venetoclax (ABT-199, GDC-0199)

製品コードS8048

Venetoclax (ABT-199, GDC-0199)化学構造

分子量(MW):868.44

Venetoclax (ABT-199, GDC-0199) is a Bcl-2-selective inhibitor with Ki of <0.01 nM in cell-free assays, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Phase 3.

サイズ 価格(税別)  
In DMSO JPY 114800
JPY 46800
JPY 163000
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バルク問合せ

文献中Selleckの製品使用例(68)

製品安全説明書

Bcl-2阻害剤の選択性比較

生物活性

製品説明 Venetoclax (ABT-199, GDC-0199) is a Bcl-2-selective inhibitor with Ki of <0.01 nM in cell-free assays, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Phase 3.
特性 Re-engineered version of ABT-263 (Navitoclax).
ターゲット
Bcl-2 [1]
(Cell-free assay)
<0.01 nM(Ki)
体外試験

ABT-199 shows less sensitivity to Bcl-xL, Mcl-1 and Bcl-w with Ki of 48 nM, > 444 nM and 245 nM, respectively. ABT-199 potently inhibits FL5.12-Bcl-2 cells, RS4;11 cells with EC50 of 4 nM and 8 nM, while shows low activity against FL5.12-Bcl-xL cells with EC50 of 261 nM. ABT-199 induces a rapid apoptosis in RS4;11 cells with cytochrome c release, caspase activation, the externalization of phosphatidylserine and the accumulation of sub-G0/G1 DNA. Quantitative immunoblotting reveals that sensitivity to ABT-199 correlated strongly with the expression of Bcl-2, including NHL, DLBCL, MCL, AML and ALL cell lines. ABT-199 also induces apoptosis in CLL with an average EC50 of 3.0 nM. [1]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CS-THL1 MmLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\0OZIzOCCwTR?= M3v0NVczKGh? NX\0V5huTE2VTx?= M{niNGlvcGmkaYTzJINmdGxiZ4Lve5RpKGG|c3Xzd4VlKGK7IHPlcIwhfmmjYnnsbZR6 MVKyOVkyPjZ7OB?=
CS-THL1 M1u4[WFxd3C2b4TpZ{BCe3OjeR?= MXmyOUBvVQ>? NFywNoFFVVOR Ml7oTY5lfWOnczDhdI9xfG:|aYO= NIjzU4YzPTlzNk[5PC=>
DoGKiT NHLI[|ZCeG:ydH;0bYMhSXO|YYm= MYq1NEBvVQ>? MoXYSG1UVw>? NXPOWJNCUW6mdXPld{BieG:ydH;zbZM> NUDRcXhpOjV7MU[2PVg>
RS4-11 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1ixNlczKGh? MV;JR|UxRTBwMESwNkDPxE1? NGLNR5IzPTZ2OUe2PC=>
NALM-6 NWX6NXF2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnV[ZdCPzJiaB?= M{PUXWlEPTB-MzFOwG0> MoTxNlU3PDl5Nki=
SU-DHL-6 M2r5bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjZe|kxNjhizszN MWrJcohq[mm2czDj[YxtKGe{b4f0bEBie3Onc4Pl[EBjgSClZXzsJJZq[WKrbHn0fS=> NU\0cHliOjV3OUC4NFM>
OCI-Ly19 NF7UXIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIi5RlcyKM7:TR?= NIjtfHhKdmirYnn0d{Bk\WyuIHfyc5d1cCCjc4Pld5Nm\CCkeTDj[YxtKH[rYXLpcIl1gQ>? MoPWNlU2QTB6MEO=
SU-DHL-6 MX3GeY5kfGmxbjDBd5NigQ>? M1PxO|AvPzVizszN MkPiNVghcA>? MnjsTY5kemWjc3XzJJBzdy2|dYL2bZZidCCycn;0[YlvKE2FTD2xJIV5eHKnc4Ppc44> MoH2NlU2QTB6MEO=
KCL22 Mkm1SpVv[3Srb36gRZN{[Xl? M{\vO|Ih|ryP NIDxOm81QCCq MmnySG1UVw>? M2DyUWlv[3KnYYPld{BFVkFiZoLh[4Fu\W62YYTpc44> NWXpbpU{OjV|M{OyOVI>
LOUCY M4TJN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DBPFExKM7:TR?= M2jDNlQ5KGh? NIflRotFVVOR MWjJR|UxRTBwMEGzPUDPxE1? NFK4O|czPTNyMUewOC=>
ALL-SIL M1q1[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUOxNEDPxE1? NYDFUFdWPDhiaB?= NYjnbHNrTE2VTx?= NEX3[5dKSzVyPUCuNVgxOyEQvF2= MYqyOVMxOTdyNB?=
CUTLL1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLrd2VlOTBizszN NU[3dY5kPDhiaB?= MYHEUXNQ MWTJR|UxRTBwM{iyN{DPxE1? M3\VcVI2OzBzN{C0
KOPTK1 NGDhWYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTONVAh|ryP NW\ZO|FGPDhiaB?= MVPEUXNQ NEjhNG9KSzVyPUCuOlQ{OiEQvF2= NUfo[3lCOjV|MEG3NFQ>
DND-41 M1nSOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrDUm4yOCEQvF2= NFvIXIM1QCCq NYLGTotFTE2VTx?= MVzJR|UxRTFwOU[5OUDPxE1? MVOyOVMxOTdyNB?=
PF-382 M1XFeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fIWFExKM7:TR?= NFjHS3o1QCCq NHK5bVRFVVOR MnLKTWM2OD1{LkG4NlQh|ryP NIK2bIYzPTNyMUewOC=>
KARPAS-45 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvjW5lROTBizszN MWm0PEBp MkD2SG1UVw>? M3P5c2lEPTB;Mz6yNlI2KM7:TR?= NWjFfIlHOjV|MEG3NFQ>
PEER NHTzV5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVKxNEDPxE1? MVq0PEBp M1:zdGROW09? NF3q[VJKSzVyPUSuOlQxOyEQvF2= NVvvW5NMOjV|MEG3NFQ>
CX-1 Mli3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTsbGcyODBizszN M2CzdVczKGh? NX3JNI5bUUN3ME22Mlch|ryP NULhWI9ZOjV{MEi4PFI>
LS147T MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHP5TpkyODBizszN NH:2OpE4OiCq NHTtfYhKSzVyPUK5MlUh|ryP M3zvSFI2OjB6OEiy
HL-60 NULXfoZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWi0PEBp MUjJR|UxRDFizszN MXOyOFM1PjFzNh?=
MOLM-13 NFGzcIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV[0PEBp NWnL[4RzUUN3MEyxJO69VQ>? MWOyOFM1PjFzNh?=
OCI-AML2 NHL0UpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXq0PEBp NHvwfFNKSzVyPEGg{txO NYnaXWl7OjR|NE[xNVY>
Kasumi-1 NF3wbGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1WwblQ5KGh? NGTvbGZKSzVyPEGg{txO MorFNlQ{PDZzMU[=
KG-1 NI\1VlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PUcVQ5KGh? MWrJR|UxRDFizszN Ml;iNlQ{PDZzMU[=
THP-1 NWnYVWRQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NID5W|U1QCCq NH\PfVRKSzVyPEGg{txO MVGyOFM1PjFzNh?=
MOLM-14 M1vvcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPkV|c1QCCq MWXJR|UxRDFizszN NFzySWgzPDN2NkGxOi=>
MOLM-13 MlnsRZBweHSxdHnjJGF{e2G7 NEjScYg2OCCwTR?= MnnuNlQhcA>? NIi1RVdCeG:ydH;zbZMhcW6mdXP0bY9v MkTMNlQ{PDZzMU[=
HSB NGXscoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV[xd41rOTBizszN MlnHOFghcA>? NEDMNIFFVVOR NETWcXVKSzVyPUSuOFQ5KM7:TR?= NWDhNYloOjR|NEK5OFg>
MOLT4 M4PVSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPMSGwyOCEQvF2= M{X2c|Q5KGh? MkHXSG1UVw>? MVXJR|UxRTRwMUW0JO69VQ>? MVOyOFM1Ojl2OB?=
SKW-3/KE-37 MnfJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M361UFExKM7:TR?= NILlWmo1QCCq NWTyVVZZTE2VTx?= MljSTWM2OD1yLkexNkDPxE1? MnnVNlQ{PDJ7NEi=
SUPT-11 NFvXbW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;WOWYyOCEQvF2= M4DTclQ5KGh? Ml3vSG1UVw>? MVfJR|UxRTRwNEezJO69VQ>? NFftdJUzPDN2Mkm0PC=>
JURKAT M3HVN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nQ[FExKM7:TR?= NWL4cmxkPDhiaB?= MWrEUXNQ MkXlTWM2OD12Lki5N{DPxE1? M4XId|I1OzR{OUS4
CCRF-CEM NWK5[YVqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3qyN|ExKM7:TR?= NUDXWnU2PDhiaB?= NYC2WnpuTE2VTx?= M4P1SGlEPTB;MT6zOlAh|ryP NUHoVYlwOjR|NEK5OFg>
LOUCY MorqRZBweHSxdHnjJGF{e2G7 M1jqXlIh|ryP MUm0PEBp NYPZVXJqTE2VTx?= NGnYeIJCeG:ydH;zbZMhcW6mdXP0bY9v MYiyOFM1Ojl2OB?=

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

アッセイ
Methods Test Index PMID
Western blot
Mcl-1 / Bcl-xl / Bcl-2 / Bak / NOXA / Bim; 

PubMed: 30663221     


A549 cells were treated with Ibr-7, ABT-199 or a combination for 2 or 4 h. Total RNA was extracted from A549 cells to undergo RT-qPCR assay.

PARP / Cleaved PARP / Caspase 3 / Cleaved caspase3 / p-S6(Ser236/236); 

PubMed: 30663221     


A549 cells were treated with Ibr-7, ABT-199 or a combination for 24 h before western blotting assay. 

30663221
Growth inhibition assay
Cell death; 

PubMed: 28714472     


The indicated cell lines, treated with 2 μM doxorubicin±1 or 2 μM ABT-199, were quantified by annexin-V staining at 24 h for H2171 and H446 or at 48 h for H196 and SW1271 (mean±s.d., n=3). 

Cell viability; 

PubMed: 29876007     


TNBC cells were cultured with the indicated doses of ABT-199 (μM) for 48 h. 

28714472 29876007
Immunofluorescence
Bcl-2 / Mcl-1; 

PubMed: 28767232     


HEK293T cells cotransfected with the plasmids. Upon transfection, DMSO carrier control, 0.5 μM ABT-199, 10 μM A1210477, or a combination of both 0.5 μM ABT-199 and 10 μM A1210447 were added to the cells. After 30 h, the cells were analyzed for GFP and RFP expression by fluorescence microscopy.

28767232
体内試験 ABT-199 (100 mg/kg) causes a maximal tumor growth inhibition of 95% and tumor growth delay of 152% in RS4;11 xenografts. ABT-199 also inhibits xenograft growth (DoHH2, Granta-519) as a single agent or in combination with SDX-105 and other agents. [1]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
+ 展開

Binding affinity assays:

Binding affinities (Ki or IC50) of ABT-199 against different isoforms of Bcl-2 family are determined with competitive fluorescence polarization assays. The following peptide probe/protein pairs are used: f-bad (1 nM) and Bcl-xL (6 nM), f-Bax (1 nM) and Bcl-2 (10 nM), f-Bax (1 nM) and Bcl-w (40 nM), f-Noxa (2 nM) and Mcl-1 (40 nM), and f-Bax (1 nM) and Bcl-2-A1 (15 nM). Binding affinities for Bcl-xL are also determined using a time-resolved fluorescence resonance energy transfer assay. Bcl-xL (1 nM, His tagged) is mixed with 200 nM f-Bak, 1 nM Tb-labeled anti-His antibody, and ABT-199 at room temperature for 30 min. Fluorescence is measured on an Envision plate reader using a 340/35 nm excitation filter and 520/525 (f-Bak) and 495/510 nm (Tb-labeled anti-His antibody) emission filters.
細胞試験: [1]
+ 展開
  • 細胞株: NHL, DLBCL, MCL, AML and ALL cell lines
  • 濃度: ~1 μM
  • 反応時間: 48 hours
  • 実験の流れ: RS4;11 cells are seeded at 5 × 104 per well in 96-well plates and treated with ABT-199 diluted in half-log steps starting at 1 μM-0.05 nM. Leukemia and lymphoma cell lines are seeded at 1.5-2 × 104 cells per well in the appropriate medium and incubated with ABT-199 for 48 h. Effects on proliferation are determined using Cell TiterGlo reagent. EC50 values are determined by nonlinear regression analysis of the concentration-response data.
    (参考用のみ)
動物試験:[1]
+ 展開
  • 動物モデル: Female C.B-17 SCID mice (DoHH2 and Granta-519 xenografts) and female C.B-17 SCID-beige mice (RS4;11 and Toledo xenografts)
  • 製剤: 60% phosal 50 propylene glycol (PG), 30% polyethylene glycol (PEG) 400 and 10% ethanol
  • 投薬量: ~100 mg/kg
  • 投与方法: Orally
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 100 mg/mL (115.14 mM) warming
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
5% DMSO+50% PEG 300+5% Tween 80+ddH2O
混合させたのち直ちに使用することを推奨します。
5mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 868.44
化学式

C45H50ClN7O7S

CAS No. 1257044-40-8
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04073147 Not yet recruiting Primary CNS Lymphoma Klinikum Stuttgart|University Hospital Freiburg November 2019 Phase 1
NCT04070768 Not yet recruiting Acute Myeloid Leukemia Big Ten Cancer Research Consortium|Pfizer|AbbVie October 2019 Phase 1
NCT03943342 Not yet recruiting Chronic Lymphocytic Leukemia|Loss of Chromosome 17p Kerry Rogers|National Cancer Institute (NCI)|Janssen Research & Development LLC|Ohio State University Comprehensive Cancer Center September 1 2019 Phase 2
NCT03900884 Not yet recruiting Breast Neoplasm Female Peter MacCallum Cancer Centre Australia September 2019 Phase 1

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問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.

  • 質問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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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID