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(2)

  • 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.

    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 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWG0d5JvOjBibl2= MmHzO|IhcA>? NFXwZmZFVVOR MlvXTY5pcWKrdIOgZ4VtdCCpcn;3eIgh[XO|ZYPz[YQh[nliY3XscEB3cWGkaXzpeJk> M{H4RlI2QTF4Nkm4
CS-THL1 MoPVRZBweHSxdHnjJGF{e2G7 MXKyOUBvVQ>? M4XmN2ROW09? M4TZWmlv\HWlZYOgZZBweHSxc3nz NHH4NpczPTlzNk[5PC=>
DoGKiT NEn5eVNCeG:ydH;0bYMhSXO|YYm= MVi1NEBvVQ>? M{T0dGROW09? NUfDfYo6UW6mdXPld{BieG:ydH;zbZM> M4npPFI2QTF4Nkm4
RS4-11 NHKycmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYP1[pZKPzJiaB?= NVWyUYlOUUN3ME2wMlA1ODJizszN MV:yOVY1QTd4OB?=
NALM-6 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTSfJBOPzJiaB?= MkTOTWM2OD5|IN88US=> Mnz2NlU3PDl5Nki=
SU-DHL-6 MkjiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVz3TGRtOC56IN88US=> M3;Xe2lvcGmkaYTzJINmdGxiZ4Lve5RpKGG|c3Xzd4VlKGK7IHPlcIwhfmmjYnnsbZR6 MUSyOVU6ODhyMx?=
OCI-Ly19 NV7xeVBQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjtNUDPxE1? MVnJcohq[mm2czDj[YxtKGe{b4f0bEBie3Onc4Pl[EBjgSClZXzsJJZq[WKrbHn0fS=> M4TtZVI2PTlyOECz
SU-DHL-6 MofZSpVv[3Srb36gRZN{[Xl? MWSwMlc2KM7:TR?= MWixPEBp M{fOS2lv[3KnYYPld{Bxem9vc4Xyeol3[WxicILveIVqdiCPQ1ytNUBmgHC{ZYPzbY9v NH\4NVAzPTV7MEiwNy=>
KCL22 MmnISpVv[3Srb36gRZN{[Xl? M4W1dVIh|ryP MXu0PEBp NULjeHN2TE2VTx?= M{nidGlv[3KnYYPld{BFVkFiZoLh[4Fu\W62YYTpc44> MXqyOVM{OzJ3Mh?=
LOUCY MlziS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonkNVAh|ryP MUe0PEBp NH3sXZVFVVOR M1j0W2lEPTB;MD6wNVM6KM7:TR?= NFXwZXEzPTNyMUewOC=>
ALL-SIL M1\FRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfqcJoyOCEQvF2= MofUOFghcA>? NX\qXVB5TE2VTx?= NFXOPIJKSzVyPUCuNVgxOyEQvF2= MXKyOVMxOTdyNB?=
CUTLL1 M2HZNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLQS4UyOCEQvF2= MoXLOFghcA>? NYfYb2JCTE2VTx?= NVL4ZXpjUUN3ME2wMlM5OjNizszN M3yxWFI2OzBzN{C0
KOPTK1 MnTvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfVXpR7OTBizszN NIq5PJE1QCCq NFfMPW1FVVOR MmfrTWM2OD1yLk[0N|Ih|ryP M175R|I2OzBzN{C0
DND-41 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFz2SocyOCEQvF2= MXS0PEBp NVv4e3Q5TE2VTx?= NYP4bVVQUUN3ME2xMlk3QTVizszN M4qyNlI2OzBzN{C0
PF-382 Ml2yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzmfVcyOCEQvF2= NE\FWmw1QCCq NFS0UpNFVVOR NF;MPFBKSzVyPUKuNVgzPCEQvF2= MmPyNlU{ODF5MES=
KARPAS-45 NEHkZ4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnINVAh|ryP NGG1UmQ1QCCq NH73T|NFVVOR NFv3OppKSzVyPUOuNlIzPSEQvF2= NX20U4N1OjV|MEG3NFQ>
PEER NV7yToJiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rOTFExKM7:TR?= M13qcFQ5KGh? MWfEUXNQ NV\0SpZ5UUN3ME20MlY1ODNizszN M1j1VFI2OzBzN{C0
CX-1 NGjqVYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rmUFExOCEQvF2= NIi1OVc4OiCq MULJR|UxRTZwNzFOwG0> NIHNUXQzPTJyOEi4Ni=>
LS147T MlSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrTNVAxKM7:TR?= NGTHPI04OiCq NG\m[JNKSzVyPUK5MlUh|ryP M2qxbFI2OjB6OEiy
HL-60 MkPCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTVdFA6PDhiaB?= M2rjSGlEPTB:MTFOwG0> M{CwNVI1OzR4MUG2
MOLM-13 NEf2T2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDaOFghcA>? MXTJR|UxRDFizszN M{\PNFI1OzR4MUG2
OCI-AML2 M4nST2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXDOFghcA>? M1fKemlEPTB:MTFOwG0> NGqycGQzPDN2NkGxOi=>
Kasumi-1 MonVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17ae|Q5KGh? MnTwTWM2ODxzIN88US=> NF\rZ2EzPDN2NkGxOi=>
KG-1 NELQNGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zGPFQ5KGh? M2nzWGlEPTB:MTFOwG0> MkDnNlQ{PDZzMU[=
THP-1 M4LsNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTKOFghcA>? NWLZXZdDUUN3MEyxJO69VQ>? NVPBOo9HOjR|NE[xNVY>
MOLM-14 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TaOVQ5KGh? NV7ZSodzUUN3MEyxJO69VQ>? MUCyOFM1PjFzNh?=
MOLM-13 NW\Gd4Z[SXCxcITveIlkKEG|c3H5 M{XMU|UxKG6P NGjxVHozPCCq NYjIOXVjSXCxcITvd4l{KGmwZIXjeIlwdg>? NUDTeo5EOjR|NE[xNVY>
HSB MlP4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPm[XEyOCEQvF2= M1fNV|Q5KGh? NH;aT4pFVVOR M4fFS2lEPTB;ND60OFgh|ryP NXnwb454OjR|NEK5OFg>
MOLT4 M2TNT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYmxNEDPxE1? NH3hVmg1QCCq MY\EUXNQ MkW1TWM2OD12LkG1OEDPxE1? MUSyOFM1Ojl2OB?=
SKW-3/KE-37 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;aUlExKM7:TR?= MV:0PEBp M4XGZmROW09? NWr3TppnUUN3ME2wMlcyOiEQvF2= MlLjNlQ{PDJ7NEi=
SUPT-11 MkfaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\Yd45vOTBizszN Mlm4OFghcA>? M2rhTmROW09? M{XmNmlEPTB;ND60O|Mh|ryP MXSyOFM1Ojl2OB?=
JURKAT NFzzNWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M322bFExKM7:TR?= NU\wcW1DPDhiaB?= NGP3OJFFVVOR MVfJR|UxRTRwOEmzJO69VQ>? MVGyOFM1Ojl2OB?=
CCRF-CEM NEn0eo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzK[Zh2OTBizszN NIOzOY01QCCq NWXl[5hHTE2VTx?= NELBbnBKSzVyPUGuN|YxKM7:TR?= NFL6XYYzPDN2Mkm0PC=>
LOUCY NFvHRYVCeG:ydH;0bYMhSXO|YYm= NUDDV|BrOiEQvF2= NHvYO3E1QCCq M1;KR2ROW09? NVnFXIpLSXCxcITvd4l{KGmwZIXjeIlwdg>? MX:yOFM1Ojl2OB?=

多くの細胞株試験データを見る場合、クリックしてください

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 左から右までの手順で、溶剤を製品に加えることです:
5% DMSO+50% PEG 300+5% Tween 80+ddH2O
5mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)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
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    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

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、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 ( 輸入 輸出 )

  • 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

マス 濃度 ボリューム 分子量

臨床試験

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

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

よくある質問(FAQ)

  • 問題1:

    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