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(6)

  • (C) OCI-AML2 cells were cultured for 1 day with or without the indicated doses of CB-839 and ABT-199; apoptosis was evaluated based on Annexin V staining. (D) MOLM-14 cells were cultured for 1 day with or without the indicated doses of CB-839 and ABT-199; apoptosis was evaluated based on Annexin-V staining. Histograms show data that are representative of 3 independent experiments. The response of the combination was compared with its single agents against the widely used Loewe model for drug-with-itself dose additivity using Chalice software26 and presented as an isobologram. *P < .05, **P < .01, ***P < .001.

    Blood, 2015, 126(11):1346-56. Venetoclax (ABT-199, GDC-0199) purchased from Selleck.

    (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 NIj0RmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\IdGUzOCCwTR?= MnvTO|IhcA>? NVr1T29KTE2VTx?= NFjkcI5KdmirYnn0d{Bk\WyuIHfyc5d1cCCjc4Pld5Nm\CCkeTDj[YxtKH[rYXLpcIl1gQ>? M2K3ZlI2QTF4Nkm4
CS-THL1 MnrQRZBweHSxdHnjJGF{e2G7 NHq5[oQzPSCwTR?= MnTISG1UVw>? MlnRTY5lfWOnczDhdI9xfG:|aYO= MWKyOVkyPjZ7OB?=
DoGKiT M3\NR2Fxd3C2b4TpZ{BCe3OjeR?= MkPXOVAhdk1? M{C4[WROW09? MYDJcoR2[2W|IHHwc5B1d3Orcx?= NF61RnYzPTlzNk[5PC=>
RS4-11 MljOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG[ybnU4OiCq NWDRS443UUN3ME2wMlA1ODJizszN M1;HV|I2PjR7N{[4
NALM-6 NFHyZVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVS3NkBp NIn2Om1KSzVyPkOg{txO MVyyOVY1QTd4OB?=
SU-DHL-6 M{TPSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYqwMlgh|ryP NX\VOoJzUW6qaXLpeJMh[2WubDDndo94fGhiYYPz[ZN{\WRiYomgZ4VtdCC4aXHibYxqfHl? Mlj1NlU2QTB6MEO=
OCI-Ly19 M4HseWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX62[nlxOSEQvF2= Mk\5TY5pcWKrdIOgZ4VtdCCpcn;3eIgh[XO|ZYPz[YQh[nliY3XscEB3cWGkaXzpeJk> NXvmZ4NPOjV3OUC4NFM>
SU-DHL-6 Mlq1SpVv[3Srb36gRZN{[Xl? M4T0OlAvPzVizszN NV7hWYpIOThiaB?= MX3JcoNz\WG|ZYOgdJJwNXO3co\peoFtKHC{b4TlbY4hVUOOLUGg[ZhxemW|c3nvci=> MUCyOVU6ODhyMx?=
KCL22 MYPGeY5kfGmxbjDBd5NigQ>? MkTwNkDPxE1? M2XXSFQ5KGh? NIjR[oRFVVOR NIqxbWhKdmO{ZXHz[ZMhTE6DIH\yZYdidWWwdHH0bY9v M3[0fVI2OzN|MkWy
LOUCY M3fmXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MniyNVAh|ryP Ml;kOFghcA>? NELPWJdFVVOR MWfJR|UxRTBwMEGzPUDPxE1? NVTLNoxUOjV|MEG3NFQ>
ALL-SIL MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV31WoZxOTBizszN MomwOFghcA>? MlLLSG1UVw>? NXq1epBnUUN3ME2wMlE5ODNizszN MYqyOVMxOTdyNB?=
CUTLL1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;KNVAh|ryP M2jWT|Q5KGh? M4XCT2ROW09? M1XibGlEPTB;MD6zPFI{KM7:TR?= NFP0RpYzPTNyMUewOC=>
KOPTK1 NGfXTo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY[xNEDPxE1? MYC0PEBp M1XRTWROW09? MluwTWM2OD1yLk[0N|Ih|ryP NIXGXGIzPTNyMUewOC=>
DND-41 M3TMemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPoeWxFOTBizszN MmHvOFghcA>? NYXUbHIxTE2VTx?= NYfaXZVMUUN3ME2xMlk3QTVizszN NHHKWGEzPTNyMUewOC=>
PF-382 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrkWYxWOTBizszN M1nzN|Q5KGh? NV3ZZVFUTE2VTx?= NE\PSItKSzVyPUKuNVgzPCEQvF2= M{L0UFI2OzBzN{C0
KARPAS-45 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPXSYpmOTBizszN NXGzTGlFPDhiaB?= MnHaSG1UVw>? M32w[2lEPTB;Mz6yNlI2KM7:TR?= MkDENlU{ODF5MES=
PEER NXzk[nE6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWOxNEDPxE1? NYLKNlBFPDhiaB?= MmXYSG1UVw>? NFPwNXFKSzVyPUSuOlQxOyEQvF2= M3;jNVI2OzBzN{C0
CX-1 NEPCNHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3nblcyODBizszN NFzDe2U4OiCq MmjGTWM2OD14Lkeg{txO MkDWNlUzODh6OEK=
LS147T NUfY[2pFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELSNXMyODBizszN MVK3NkBp M3i3SWlEPTB;MkmuOUDPxE1? MXeyOVIxQDh6Mh?=
HL-60 MlT1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XyOlQ5KGh? MoL4TWM2ODxzIN88US=> MWWyOFM1PjFzNh?=
MOLM-13 NHTrW|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nPS|Q5KGh? M1j2dWlEPTB:MTFOwG0> M4jIU|I1OzR4MUG2
OCI-AML2 NXL3e2d{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PoVlQ5KGh? NWPmfGpyUUN3MEyxJO69VQ>? MXmyOFM1PjFzNh?=
Kasumi-1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkW4OFghcA>? MmHrTWM2ODxzIN88US=> MUGyOFM1PjFzNh?=
KG-1 NVv6SVR1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLCcmw6PDhiaB?= NED1WnpKSzVyPEGg{txO MkiyNlQ{PDZzMU[=
THP-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHzOFghcA>? MW\JR|UxRDFizszN NYnUOVN3OjR|NE[xNVY>
MOLM-14 M1TmeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fxVVQ5KGh? M17QZ2lEPTB:MTFOwG0> M17DXVI1OzR4MUG2
MOLM-13 MVLBdI9xfG:2aXOgRZN{[Xl? MnO1OVAhdk1? M2jqeVI1KGh? NV7uT5lXSXCxcITvd4l{KGmwZIXjeIlwdg>? MV6yOFM1PjFzNh?=
HSB MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPjNVAh|ryP NUGwbmV7PDhiaB?= M{PxOWROW09? NIC4dJJKSzVyPUSuOFQ5KM7:TR?= Ml;kNlQ{PDJ7NEi=
MOLT4 MmrBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXYNVAh|ryP MofjOFghcA>? NX;ubGwxTE2VTx?= Ml\4TWM2OD12LkG1OEDPxE1? NX[2dol7OjR|NEK5OFg>
SKW-3/KE-37 M3LnU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYWxNEDPxE1? MYm0PEBp NHHRR2NFVVOR NETY[oxKSzVyPUCuO|EzKM7:TR?= MUCyOFM1Ojl2OB?=
SUPT-11 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzsNI5[OTBizszN MVK0PEBp MV7EUXNQ NF\OZYhKSzVyPUSuOFc{KM7:TR?= MWSyOFM1Ojl2OB?=
JURKAT MlHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYixNEDPxE1? NEjYRpA1QCCq MkfOSG1UVw>? NUfBZXA5UUN3ME20Mlg6OyEQvF2= MY[yOFM1Ojl2OB?=
CCRF-CEM M{fnU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NES3VXUyOCEQvF2= NHTBXGo1QCCq NEPjfZhFVVOR NVT3dJJWUUN3ME2xMlM3OCEQvF2= M1vQXFI1OzR{OUS4
LOUCY M{X2V2Fxd3C2b4TpZ{BCe3OjeR?= NHrmbnczKM7:TR?= NVL5XHZYPDhiaB?= MnTwSG1UVw>? MkPCRZBweHSxc3nzJIlv\HWldHnvci=> MXqyOFM1Ojl2OB?=

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
NCT03872180 Not yet recruiting CCND1 Positive|Mantle Cell Lymphoma|t(11;14) Positive Emory University|Genentech Inc. March 1 2020 Phase 2
NCT03872180 Not yet recruiting CCND1 Positive|Mantle Cell Lymphoma|t(11;14) Positive Emory University|Genentech Inc. March 1 2020 Phase 2
NCT03884972 Not yet recruiting Refractory Chronic Lymphocytic Leukemia|Refractory Small Lymphocytic Lymphoma M.D. Anderson Cancer Center|National Cancer Institute (NCI) December 1 2019 Phase 1
NCT03884972 Not yet recruiting Refractory Chronic Lymphocytic Leukemia|Refractory Small Lymphocytic Lymphoma M.D. Anderson Cancer Center|National Cancer Institute (NCI) December 1 2019 Phase 1
NCT03868722 Not yet recruiting CLL Rigshospitalet Denmark|Stichting Hemato-Oncologie voor Volwassenen Nederland|Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA)|Karolinska Institutet August 1 2019 Phase 2|Phase 3
NCT03868722 Not yet recruiting CLL Rigshospitalet Denmark|Stichting Hemato-Oncologie voor Volwassenen Nederland|Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA)|Karolinska Institutet August 1 2019 Phase 2|Phase 3

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