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)  
JPY 112880.00
JPY 44820.00
JPY 161020.00

カスタマーフィードバック(5)

  • (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.

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 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVGyNEBvVQ>? M1jzb|czKGh? NVjFNZhrTE2VTx?= NWLQPHdwUW6qaXLpeJMh[2WubDDndo94fGhiYYPz[ZN{\WRiYomgZ4VtdCC4aXHibYxqfHl? NFu0VYUzPTlzNk[5PC=>
CS-THL1 NX7IU3A1SXCxcITveIlkKEG|c3H5 NVvOclQ3OjVibl2= MnvhSG1UVw>? MUHJcoR2[2W|IHHwc5B1d3Orcx?= MVeyOVkyPjZ7OB?=
DoGKiT M3K5b2Fxd3C2b4TpZ{BCe3OjeR?= NIjINIk2OCCwTR?= NIjqOmdFVVOR Mmn5TY5lfWOnczDhdI9xfG:|aYO= M3vJb|I2QTF4Nkm4
RS4-11 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LoeFczKGh? MVTJR|UxRTBwMESwNkDPxE1? NVT4dFJMOjV4NEm3Olg>
NALM-6 NYLlUHVyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHOO|IhcA>? NYfRR4NVUUN3ME6zJO69VQ>? MXmyOVY1QTd4OB?=
SU-DHL-6 M1H2fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fqb|AvQCEQvF2= NEjCVnRKdmirYnn0d{Bk\WyuIHfyc5d1cCCjc4Pld5Nm\CCkeTDj[YxtKH[rYXLpcIl1gQ>? MUSyOVU6ODhyMx?=
OCI-Ly19 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVKxJO69VQ>? MXvJcohq[mm2czDj[YxtKGe{b4f0bEBie3Onc4Pl[EBjgSClZXzsJJZq[WKrbHn0fS=> MVeyOVU6ODhyMx?=
SU-DHL-6 M4[4d2Z2dmO2aX;uJGF{e2G7 NELsOI0xNjd3IN88US=> NHrvRXEyQCCq NXHkUJFkUW6lcnXhd4V{KHC{bz3zeZJ3cX[jbDDwdo91\WmwIF3DUE0yKGW6cILld5Nqd25? MlX5NlU2QTB6MEO=
KCL22 MW\GeY5kfGmxbjDBd5NigQ>? MlnuNkDPxE1? NYD4ZWZWPDhiaB?= M2jRUWROW09? MUfJcoNz\WG|ZYOgSG5CKG[{YXfhcYVvfGG2aX;u NIX2W|AzPTN|M{K1Ni=>
LOUCY NXq0PXJ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4Gz[FExKM7:TR?= MWW0PEBp NH\nem1FVVOR NFzOdJBKSzVyPUCuNFE{QSEQvF2= M4T5PVI2OzBzN{C0
ALL-SIL MnfnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEj6XXIyOCEQvF2= M1u0TFQ5KGh? NWfyc|FsTE2VTx?= MXXJR|UxRTBwMUiwN{DPxE1? NV\2b4FqOjV|MEG3NFQ>
CUTLL1 M1Szfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\tUI82OTBizszN MnPtOFghcA>? MX\EUXNQ M4\QOWlEPTB;MD6zPFI{KM7:TR?= NYXSfIRHOjV|MEG3NFQ>
KOPTK1 NGLFZnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzqd3FXOTBizszN MorMOFghcA>? MYDEUXNQ MXfJR|UxRTBwNkSzNkDPxE1? NHzGW5IzPTNyMUewOC=>
DND-41 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\5[ogyOCEQvF2= M3PLWFQ5KGh? M376emROW09? Ml7hTWM2OD1zLkm2PVUh|ryP MmDsNlU{ODF5MES=
PF-382 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWexNEDPxE1? NWG0UG44PDhiaB?= M{XrcmROW09? M3jrZ2lEPTB;Mj6xPFI1KM7:TR?= NFPlO2kzPTNyMUewOC=>
KARPAS-45 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPwNVAh|ryP MWK0PEBp M2myPWROW09? NIrBSllKSzVyPUOuNlIzPSEQvF2= MYGyOVMxOTdyNB?=
PEER M2fUWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jDTlExKM7:TR?= MWS0PEBp MV;EUXNQ M1HPRWlEPTB;ND62OFA{KM7:TR?= MkPjNlU{ODF5MES=
CX-1 NH[zPYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfrNVAxKM7:TR?= M4SyN|czKGh? MonLTWM2OD14Lkeg{txO MnKyNlUzODh6OEK=
LS147T MlW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjsNVAxKM7:TR?= M4fPUVczKGh? M3P3PWlEPTB;MkmuOUDPxE1? M4LHdVI2OjB6OEiy
HL-60 NFzLclZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUS0PEBp NFXCTllKSzVyPEGg{txO MmjFNlQ{PDZzMU[=
MOLM-13 Mm\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vaZlQ5KGh? NInUdHNKSzVyPEGg{txO M3nQZVI1OzR4MUG2
OCI-AML2 MmD6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGftRpY1QCCq MUHJR|UxRDFizszN NY\vOZNzOjR|NE[xNVY>
Kasumi-1 M1nuVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXq0PEBp NXHZ[25YUUN3MEyxJO69VQ>? NFHSW4gzPDN2NkGxOi=>
KG-1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVe0PEBp NWPlOYdIUUN3MEyxJO69VQ>? M1vmfVI1OzR4MUG2
THP-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknEOFghcA>? NVHOW3NtUUN3MEyxJO69VQ>? M2jwUVI1OzR4MUG2
MOLM-14 M2\Vb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DRSVQ5KGh? NG\mfoZKSzVyPEGg{txO NWD4XpF[OjR|NE[xNVY>
MOLM-13 NYXhe4FYSXCxcITveIlkKEG|c3H5 NEDRZYU2OCCwTR?= NFnBUVIzPCCq NUHKTYxCSXCxcITvd4l{KGmwZIXjeIlwdg>? MkTmNlQ{PDZzMU[=
HSB M2HIc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnqUm4yOCEQvF2= M4jnb|Q5KGh? MVzEUXNQ NG\Ge2RKSzVyPUSuOFQ5KM7:TR?= MX6yOFM1Ojl2OB?=
MOLT4 NXuwU3E{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVKxNEDPxE1? MXK0PEBp M4PxcWROW09? Mmf2TWM2OD12LkG1OEDPxE1? MlPHNlQ{PDJ7NEi=
SKW-3/KE-37 MkPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXz2d4cxOTBizszN MYC0PEBp NUnhR5dyTE2VTx?= Mn\oTWM2OD1yLkexNkDPxE1? MYiyOFM1Ojl2OB?=
SUPT-11 NHvBWnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DtSFExKM7:TR?= Mk[0OFghcA>? MnT5SG1UVw>? MUXJR|UxRTRwNEezJO69VQ>? MYOyOFM1Ojl2OB?=
JURKAT NXHwb5g3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWWxNEDPxE1? MmXHOFghcA>? M4\NcWROW09? MY\JR|UxRTRwOEmzJO69VQ>? MmXYNlQ{PDJ7NEi=
CCRF-CEM MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXSbmoyOCEQvF2= NFTPXFU1QCCq NF;XUnBFVVOR NFzRc3lKSzVyPUGuN|YxKM7:TR?= NV;HU2M1OjR|NEK5OFg>
LOUCY MVXBdI9xfG:2aXOgRZN{[Xl? NUTlXoFIOiEQvF2= M{i4R|Q5KGh? M3HQTmROW09? NV7Lc3duSXCxcITvd4l{KGmwZIXjeIlwdg>? Mo[2NlQ{PDJ7NEi=

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

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
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