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 NHfUeIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnUUYlVOjBibl2= NEDqO4o4OiCq MYHEUXNQ NUTFeZpjUW6qaXLpeJMh[2WubDDndo94fGhiYYPz[ZN{\WRiYomgZ4VtdCC4aXHibYxqfHl? NFXmdIEzPTlzNk[5PC=>
CS-THL1 Mm\CRZBweHSxdHnjJGF{e2G7 MUSyOUBvVQ>? MlT5SG1UVw>? NHXoOY9KdmS3Y3XzJIFxd3C2b4Ppdy=> NEHxNoczPTlzNk[5PC=>
DoGKiT M3X5e2Fxd3C2b4TpZ{BCe3OjeR?= NFXpZZA2OCCwTR?= NYK2WGhXTE2VTx?= NFLuXJVKdmS3Y3XzJIFxd3C2b4Ppdy=> NYq1bpE4OjV7MU[2PVg>
RS4-11 NX3GWGl[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3qUpJ[PzJiaB?= NV\ZOXRUUUN3ME2wMlA1ODJizszN MV[yOVY1QTd4OB?=
NALM-6 MkTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTaO|IhcA>? MkXFTWM2OD5|IN88US=> NUDkeG9jOjV4NEm3Olg>
SU-DHL-6 Ml6xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnz3NE45KM7:TR?= MXzJcohq[mm2czDj[YxtKGe{b4f0bEBie3Onc4Pl[EBjgSClZXzsJJZq[WKrbHn0fS=> MmjVNlU2QTB6MEO=
OCI-Ly19 NE\xdXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7DNUDPxE1? NWDoWm1KUW6qaXLpeJMh[2WubDDndo94fGhiYYPz[ZN{\WRiYomgZ4VtdCC4aXHibYxqfHl? M4PWVVI2PTlyOECz
SU-DHL-6 MmXPSpVv[3Srb36gRZN{[Xl? M3nkR|AvPzVizszN NEDkb4YyQCCq Ml;6TY5kemWjc3XzJJBzdy2|dYL2bZZidCCycn;0[YlvKE2FTD2xJIV5eHKnc4Ppc44> NVfoe3ZVOjV3OUC4NFM>
KCL22 NWLO[3hlTnWwY4Tpc44hSXO|YYm= NUXhcnNwOiEQvF2= Mn7zOFghcA>? MUDEUXNQ NY\ySmhOUW6lcnXhd4V{KESQQTDmdoFo[W2nboTheIlwdg>? NUTGRWdROjV|M{OyOVI>
LOUCY M{XYWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TSe|ExKM7:TR?= M4XDUFQ5KGh? NED4dVRFVVOR NFnYXXRKSzVyPUCuNFE{QSEQvF2= NYrNWWpYOjV|MEG3NFQ>
ALL-SIL NH3BNVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn[1NVAh|ryP M4jJT|Q5KGh? MXLEUXNQ NHTQWJRKSzVyPUCuNVgxOyEQvF2= NWrzXGZjOjV|MEG3NFQ>
CUTLL1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jpelExKM7:TR?= M1XoZVQ5KGh? NF24V5VFVVOR NYfBO2FZUUN3ME2wMlM5OjNizszN NHrrR20zPTNyMUewOC=>
KOPTK1 NGPVe|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVWxNEDPxE1? MoXxOFghcA>? MoTmSG1UVw>? NH;veJBKSzVyPUCuOlQ{OiEQvF2= MXyyOVMxOTdyNB?=
DND-41 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljHNVAh|ryP MXW0PEBp NYjBXFg6TE2VTx?= MV\JR|UxRTFwOU[5OUDPxE1? MkSwNlU{ODF5MES=
PF-382 M2n3SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonMNVAh|ryP MkTzOFghcA>? MnvnSG1UVw>? NV[4Xmg6UUN3ME2yMlE5OjRizszN NHL0bZczPTNyMUewOC=>
KARPAS-45 NHPzVZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHLO3RROTBizszN MVm0PEBp MVPEUXNQ NXP2fYRZUUN3ME2zMlIzOjVizszN NX7EXJpZOjV|MEG3NFQ>
PEER NV;SfnBFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnhUHMyOCEQvF2= NYP6dHFTPDhiaB?= NWrVbJh7TE2VTx?= Mmn4TWM2OD12Lk[0NFMh|ryP MVuyOVMxOTdyNB?=
CX-1 NY\YfIdQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUixNFAh|ryP MlLlO|IhcA>? MWHJR|UxRTZwNzFOwG0> NWTSOY9YOjV{MEi4PFI>
LS147T NX;iOpR4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknjNVAxKM7:TR?= MXO3NkBp Mm\ZTWM2OD1{OT61JO69VQ>? M{XWRVI2OjB6OEiy
HL-60 MnXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PJdlQ5KGh? MoPNTWM2ODxzIN88US=> NXXWSHp7OjR|NE[xNVY>
MOLM-13 NYK4VWtsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLEOFghcA>? NEXScFhKSzVyPEGg{txO M2fUU|I1OzR4MUG2
OCI-AML2 NHTxOYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MneyOFghcA>? NHLrSYFKSzVyPEGg{txO NFjuTJMzPDN2NkGxOi=>
Kasumi-1 Mk\kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHVcFA1QCCq M4n3dmlEPTB:MTFOwG0> MlvqNlQ{PDZzMU[=
KG-1 NYHVbIQxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1v5Z|Q5KGh? MlGzTWM2ODxzIN88US=> MoLkNlQ{PDZzMU[=
THP-1 MoXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHP1Oos1QCCq NGWzeIFKSzVyPEGg{txO NV\ySnFzOjR|NE[xNVY>
MOLM-14 M3zlZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\VO2E1QCCq MVLJR|UxRDFizszN NXPzRnc3OjR|NE[xNVY>
MOLM-13 NHfzc4JCeG:ydH;0bYMhSXO|YYm= MYW1NEBvVQ>? NWLkcpVqOjRiaB?= NWTSN5ROSXCxcITvd4l{KGmwZIXjeIlwdg>? NUe3SYs4OjR|NE[xNVY>
HSB MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDDPXB2OTBizszN Mkf2OFghcA>? NIX6PGdFVVOR MmjwTWM2OD12LkS0PEDPxE1? NYXTWmFYOjR|NEK5OFg>
MOLT4 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3pWZNMOTBizszN MkDTOFghcA>? NULufGI4TE2VTx?= NFvi[VFKSzVyPUSuNVU1KM7:TR?= MUKyOFM1Ojl2OB?=
SKW-3/KE-37 NWPrO4tVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7xbI1bOTBizszN M4KxT|Q5KGh? NGPoVW1FVVOR NH;RdXJKSzVyPUCuO|EzKM7:TR?= M4LxWFI1OzR{OUS4
SUPT-11 NWXnN4xrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDyWYQyOCEQvF2= MV[0PEBp MW\EUXNQ M4SyWWlEPTB;ND60O|Mh|ryP NXnJc5dDOjR|NEK5OFg>
JURKAT NVO0U2ZGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnlNVAh|ryP NHfYNno1QCCq Ml;5SG1UVw>? MnXDTWM2OD12Lki5N{DPxE1? NHzQWmczPDN2Mkm0PC=>
CCRF-CEM NVLHbnNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHMT|c{OTBizszN MneyOFghcA>? NFL5ZolFVVOR MXLJR|UxRTFwM{[wJO69VQ>? MW[yOFM1Ojl2OB?=
LOUCY M3\2N2Fxd3C2b4TpZ{BCe3OjeR?= NIjsUoUzKM7:TR?= NGH1WG01QCCq M{D4XmROW09? M1rENWFxd3C2b4Ppd{BqdmS3Y4Tpc44> MknSNlQ{PDJ7NEi=

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(NMPから)右の順に溶剤を製品に加えます:
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
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