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(3)

  • 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 M3f5bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH33[2UzOCCwTR?= MmTZO|IhcA>? MWfEUXNQ NEHYZWRKdmirYnn0d{Bk\WyuIHfyc5d1cCCjc4Pld5Nm\CCkeTDj[YxtKH[rYXLpcIl1gQ>? MV6yOVkyPjZ7OB?=
CS-THL1 NETWVpNCeG:ydH;0bYMhSXO|YYm= MVqyOUBvVQ>? NUm1WpB4TE2VTx?= NXH0SZQ3UW6mdXPld{BieG:ydH;zbZM> NYLw[XVbOjV7MU[2PVg>
DoGKiT MWXBdI9xfG:2aXOgRZN{[Xl? M{nHXFUxKG6P NYWxeVhwTE2VTx?= NY\aXWdzUW6mdXPld{BieG:ydH;zbZM> MXyyOVkyPjZ7OB?=
RS4-11 NIH2Z4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYS3NkBp Mm\uTWM2OD1yLkC0NFIh|ryP NXjCVVFYOjV4NEm3Olg>
NALM-6 NETpe4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjpcpY4OiCq MUXJR|UxRjNizszN MoDaNlU3PDl5Nki=
SU-DHL-6 NXKzOZZGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorvNE45KM7:TR?= NGnCWnhKdmirYnn0d{Bk\WyuIHfyc5d1cCCjc4Pld5Nm\CCkeTDj[YxtKH[rYXLpcIl1gQ>? NF;C[Y4zPTV7MEiwNy=>
OCI-Ly19 M2XVSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknBNUDPxE1? NHXZ[mhKdmirYnn0d{Bk\WyuIHfyc5d1cCCjc4Pld5Nm\CCkeTDj[YxtKH[rYXLpcIl1gQ>? NGLzUlYzPTV7MEiwNy=>
SU-DHL-6 NV3qOFU6TnWwY4Tpc44hSXO|YYm= NHvKPWYxNjd3IN88US=> Ml\wNVghcA>? NWrPfGJuUW6lcnXhd4V{KHC{bz3zeZJ3cX[jbDDwdo91\WmwIF3DUE0yKGW6cILld5Nqd25? M1vzclI2PTlyOECz
KCL22 NF7XbJBHfW6ldHnvckBCe3OjeR?= NVnxUnNIOiEQvF2= MlHiOFghcA>? MXHEUXNQ M4HMXWlv[3KnYYPld{BFVkFiZoLh[4Fu\W62YYTpc44> NFfBO2ozPTN|M{K1Ni=>
LOUCY NWOxVnhHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnS4NVAh|ryP NHXGRYo1QCCq MojhSG1UVw>? NFvWe|NKSzVyPUCuNFE{QSEQvF2= MYWyOVMxOTdyNB?=
ALL-SIL MorpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjFcYoyOCEQvF2= NVrMUY12PDhiaB?= NGC3fllFVVOR NHL0T4hKSzVyPUCuNVgxOyEQvF2= Mnr4NlU{ODF5MES=
CUTLL1 NGfESWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYO1dVlPOTBizszN MWW0PEBp MlTsSG1UVw>? M{fPbmlEPTB;MD6zPFI{KM7:TR?= NG\CW4wzPTNyMUewOC=>
KOPTK1 Mn;ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYqxNEDPxE1? NIfLUVk1QCCq NHL1RZRFVVOR M4LLbGlEPTB;MD62OFMzKM7:TR?= M4n1PFI2OzBzN{C0
DND-41 NXv1[pdPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfteGMyOCEQvF2= NHTYcGg1QCCq NVTBcXNkTE2VTx?= MX;JR|UxRTFwOU[5OUDPxE1? MnjYNlU{ODF5MES=
PF-382 M4GzXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\nSmMyOCEQvF2= M4DYelQ5KGh? NHT1dHpFVVOR Mn\RTWM2OD1{LkG4NlQh|ryP MV2yOVMxOTdyNB?=
KARPAS-45 Ml\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHHelY3OTBizszN MnPmOFghcA>? NIXKOIdFVVOR MXrJR|UxRTNwMkKyOUDPxE1? M2PRe|I2OzBzN{C0
PEER NXK2e3J3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTyNVAh|ryP M4rjXFQ5KGh? NXewNZhTTE2VTx?= M4DMS2lEPTB;ND62OFA{KM7:TR?= MYKyOVMxOTdyNB?=
CX-1 NWTOVXptT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPGNVAxKM7:TR?= NFuyOm84OiCq M{nQ[GlEPTB;Nj63JO69VQ>? MUmyOVIxQDh6Mh?=
LS147T NVHzcpF3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWD1UpRmOTByIN88US=> M1jHUVczKGh? MYnJR|UxRTJ7LkWg{txO MnvuNlUzODh6OEK=
HL-60 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jEWVQ5KGh? MkLvTWM2ODxzIN88US=> NVztbYdKOjR|NE[xNVY>
MOLM-13 M1TXfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXmOFghcA>? MWLJR|UxRDFizszN MkDmNlQ{PDZzMU[=
OCI-AML2 MnP6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrafpo1QCCq M1u1SmlEPTB:MTFOwG0> NIjQeGUzPDN2NkGxOi=>
Kasumi-1 NF6zOY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXe0PEBp MV3JR|UxRDFizszN NHG3eo0zPDN2NkGxOi=>
KG-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrqOFghcA>? M4q1OGlEPTB:MTFOwG0> M4LU[lI1OzR4MUG2
THP-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13VNFQ5KGh? NUjKZZVbUUN3MEyxJO69VQ>? M1zXbFI1OzR4MUG2
MOLM-14 Mn\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\BW|Q5KGh? MlTITWM2ODxzIN88US=> MX6yOFM1PjFzNh?=
MOLM-13 MYjBdI9xfG:2aXOgRZN{[Xl? NX3yNG15PTBibl2= Mm\4NlQhcA>? MnmyRZBweHSxc3nzJIlv\HWldHnvci=> NGnod|AzPDN2NkGxOi=>
HSB MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVGxNEDPxE1? M3G4UVQ5KGh? NF34eolFVVOR MXHJR|UxRTRwNES4JO69VQ>? Ml6zNlQ{PDJ7NEi=
MOLT4 NGnaXI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPqR4QyOCEQvF2= NIDMVmg1QCCq MlWySG1UVw>? NIrSXW9KSzVyPUSuNVU1KM7:TR?= MUWyOFM1Ojl2OB?=
SKW-3/KE-37 NGX3SY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHoXHIyOCEQvF2= NES3ZmY1QCCq M2fFPGROW09? MX7JR|UxRTBwN{GyJO69VQ>? MmWxNlQ{PDJ7NEi=
SUPT-11 NEPV[ndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYCweHNYOTBizszN NILjNIY1QCCq MVnEUXNQ MWjJR|UxRTRwNEezJO69VQ>? M1W5PVI1OzR{OUS4
JURKAT M3jxbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU[xNEDPxE1? NWHMSVJyPDhiaB?= MV;EUXNQ MnWxTWM2OD12Lki5N{DPxE1? M1nMTVI1OzR{OUS4
CCRF-CEM MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3INVAh|ryP Ml3TOFghcA>? NGnrXppFVVOR NWjXUox[UUN3ME2xMlM3OCEQvF2= NUTKUXNnOjR|NEK5OFg>
LOUCY MorHRZBweHSxdHnjJGF{e2G7 NVfUZplNOiEQvF2= MWW0PEBp NHf2SFNFVVOR NFTEeIhCeG:ydH;zbZMhcW6mdXP0bY9v MoDvNlQ{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
NCT03557619 Not yet recruiting Hematologic Malignancies AbbVie November 9 2018 Phase 1
NCT03583424 Recruiting Hematopoietic Cell Transplantation Recipient|Recurrent Diffuse Large B-Cell Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Marginal Zone Lymphoma|Recurrent Non-Hodgkin Lymphoma|Refractory Diffuse Large B-Cell Lymphoma|Refractory Follicular Lymphoma|Refractory Marginal Zone Lymphoma|Refractory Non-Hodgkin Lymphoma|Refractory Transformed Indolent Non-Hodgkin Lymphoma Ohio State University Comprehensive Cancer Center|National Cancer Institute (NCI) July 9 2018 Phase 1|Phase 2
NCT03223610 Recruiting Lymphoma|Non-Hodgkin Lymphoma|Diffuse Large B-Cell Lymphoma|Burkitt Lymphoma National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) February 9 2018 Phase 1
NCT03236857 Recruiting Malignancies|Acute Lymphoblastic Leukemia (ALL)|Acute Myeloid Leukemia (AML)|Non-Hodgkin''s Lymphoma|Neuroblastoma AbbVie|Roche-Genentech November 9 2017 Phase 1
NCT02611323 Recruiting Non-Hodgkin''s Lymphoma Hoffmann-La Roche March 9 2016 Phase 1
NCT03054896 Recruiting Richter Syndrome Dana-Farber Cancer Institute|Genentech Inc. March 8 2017 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