ABT-737

Catalog No.S1002

ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. Phase 2.

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ABT-737 Chemical Structure

ABT-737 Chemical Structure
Molecular Weight: 813.43

Validation & Quality Control

Cited by 88 publications:

14 customer reviews :

Quality Control & MSDS

Related Compound Libraries

ABT-737 is available in the following compound libraries:

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  • Bcl-2 Inhibitor in Clinical Trial

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  • Newest Bcl-2 Family Activator

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Product Information

  • Compare Bcl-2 Inhibitors
    Compare Bcl-2 Products
  • Research Area
  • Inhibition Profile
  • ABT-737 Mechanism
  • Combination Therapy
    Combination Therapy

Product Description

Biological Activity

Description ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. Phase 2.
Targets Bcl-2 [1]
(Cell-free assay)
Bcl-xL [1]
(Cell-free assay)
Bcl-w [1]
(Cell-free assay)
Bcl-B [1]
(Cell-free assay)

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IC50 30.3 nM(EC50) 78.7 nM(EC50) 197.8 nM(EC50) 1.82 μM(EC50)
In vitro ABT-737 shows low activity to Bcl-B and no effects to Mcl-1 and BFL-1. ABT-737 is sensitive to HL60, KG1 and NB4 cells with IC50 of 50 nM, 80 nM and 80 nM, respectively. ABT-737 induces apoptosis in HL60 cells, which due to decreased Bcl-2/Bax heterodimerization and has no effect on cell cycle distribution. ABT-737 also induces cytochrome c release from purified mitochondria and promotes conformational changes in Bax that are associated with apoptosis. [1] Resistant cells (Hela and MCF-7) can be sensitized to ABT-737 by approaches that down-regulate, destabilize, or inactivate Mcl-1. ABT-737 also causes Bax/BAK-dependent cytochrome c release only when Mcl-1 has been neutralized. [2] ABT-737 displaces Bim from Bcl2's BH3-binding pocket, allowing Bim to activate Bax, induce mitochondrial permeabilization, and rapidly commit the primary chronic lymphocytic leukemia (CLL) cells to death. [3] Knockdown of Mcl-1 with siRNA sensitizes two resistant SCLC cell lines H196 and DMS114 to ABT-737 by enhancing the induction of apoptosis. Likewise, up-regulation of Noxa sensitizes H196 cells to ABT-737. ABT-737 inhibits proliferation and induces apoptosis in many SCLC cell lines including NCI-H889, NCI-H1963, NCI-H1417, NCI-H146 and etc. Bcl-2 and Noxa may contribute mechanistically to the cellular response to ABT-737 in NCI-H146 cells. [4] A recent study shows that ABT-737 significantly induces apoptosis in HTLV-1 infected T-cell lines as well as in fresh ATLL cells. [5]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
OCI-Ly1 MlfPR4VtdCCYaXHibYxqfHliQYPzZZk>M3fGR|I2OCCwTdMgNEPRSGI4OiCqNHXFXVZFVVORM2DC[YNifXOnZDC5O{UhdG:|czDv[kB3cWGkaXzpeJkhcW5iY3XscJMhfHKjboPm[YN1\WRid3n0bEBDS0x4IIPpVm5CM13jelI3PjV5Mki4
KG1aMoTaR4VtdCCYaXHibYxqfHliQYPzZZk>NXrDNmlbOC1zMDFOwG0>MXuyOEBpMnjSSG1UVw>?MXvJR|UxRTdwNkig{txONCCmZXPy[YF{\XNiY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI>NGOweY8zPjV3MkexNi=>
Kasumi-1MmDaR4VtdCCYaXHibYxqfHliQYPzZZk>M4HUZ|AuOTBizszNMkHrNlQhcA>?NVjxeWgyTE2VTx?=MXPJR|UxRTRwOEeg{txONCCmZXPy[YF{\XNiY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI>MlrsNlY2PTJ5MUK=
KG1aMWHBdI9xfG:|aYOgRZN{[Xl?NGD2RowxNTFyIN88US=>NFrNcI8zPCCqNEXze3NFVVORMWfpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzNH\BWngzPjV3MkexNi=>
Kasumi-1Ml\WRZBweHSxc3nzJGF{e2G7M{P0VFAuOTBizszNMWSyOEBpMYDEUXNQNX7KO3locW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?=MW[yOlU2OjdzMh?=
MC-3 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NYDuS4lzPS9zMD:yNEDPxE1?NXjtWmJOOjRiaB?=Mn22SG1UVw>?NVjzXnBEcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?NIjGXoszPjR2N{[xOS=>
HN22 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MUSyMlUwPy53L{KyMlUh|ryPMn;yNlQhcA>?NUHRVnN5TE2VTx?=M4LmOYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzMnvmNlY1PDd4MUW=
MC-3 NILzPXlCeG:ydH;zbZMhSXO|YYm=NITCTmU2NzFyL{KwJO69VQ>?M1nQU|I1KGh?M3vrN2ROW09?M1vrSIlv\HWlZYOgZ4F{eGG|ZT3t[YRq[XSnZDDhdI9xfG:|aYO=MonLNlY1PDd4MUW=
HN22 NWKxUYdMSXCxcITvd4l{KEG|c3H5MkXJNk42NzdwNT:yNk42KM7:TR?=NHXEOlIzPCCqNV;heYFwTE2VTx?=NF\NN|VqdmS3Y3XzJINie3Cjc3WtcYVlcWG2ZXSgZZBweHSxc3nzMofvNlY1PDd4MUW=
MOLT-4M2PSfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M4\0cVExNTVyMECgcm0>NUjXWJZQPzJiaB?=MWXEUXNQM{TyfmlEPTB;MD6xPVgh|ryPMoLiNlY{QTJ|M{K=
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CEM RNIDwUHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M1:xflExNTVyMECgcm0>NHPYeVQ4OiCqMnvhSG1UVw>?M3vsW2lEPTB;NT60JO69VQ>?MVqyOlM6OjN|Mh?=
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CEM SMoLJRZBweHSxc3nzJGF{e2G7MYqxNE0yODByIH7NNEfFZYQzPCCqMVvEUXNQMkfwZ4F2e2W|IITo[UBkdGWjdnHn[UBw\iCEY3ytNkBidmRidHjlJIRwf26{ZXf1cIF1cW:wIH;mJGJkdC26TDDhcoQhVWOuLUG=NIH3NXAzPjN7MkOzNi=>
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B16M{L1Z2NmdGxiVnnhZoltcXS7IFHzd4F6MYGxNFDDqG6PMUi3NkBpM{jQeoVvcGGwY3XzJIN2emO3bXnuMYlv\HWlZXSgZY51cS2|dYL2bZZidMLiM4G0UFI3OTF4N{e2
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MOLM-13 NWTHS|hsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MVW3NkBpNUPkW2pOUUN3MNMgQUAzPy57IH7NMUKyOlA1PTZyOR?=
OCI-AML3MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MXW3NkBpMmDYTWM2OMLiPTCxPVUxKG6PMWWyOlA1PTZyOR?=
BCWM.1NFvXUnZCeG:ydH;zbZMhSXO|YYm=MX:wMVEvPiEQvF2=NG\ZeYQzPCCqNEjiS2dqdmS3Y3XzJINmdGxiYYDvdJRwe2m|MlrINlU5QTN{OUC=
MWCL-1NVWxSphzSXCxcITvd4l{KEG|c3H5NW\TdohQOC1zLk[g{txONF\SXpgzPCCqNXLhfWFYcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?=NFHsfHYzPTh7M{K5NC=>
MM.1sNUnzSI5qSXCxcITvd4l{KEG|c3H5NEnoU|YxNTFwNjFOwG0>MlixNlQhcA>?M{PXVYlv\HWlZYOgZ4VtdCCjcH;weI9{cXN?MUWyOVg6OzJ7MB?=
HCT116MmfPSpVv[3Srb36gRZN{[Xl?NEjMXI4{NzFyIN88US=>NHnz[|kyOsLiaNMgMUHEUXNQNEn6UmxqdmS3Y3XzJIEh\G:|ZT3k[ZBmdmSnboSgbY5kemWjc3WgbY4hVEN|Qj3JTUBkd264ZYLzbY9vKGGwZDDTVXNVVTFiZHXndoFl[XSrb36=M1zaUVI2PzF3MEK4
HCT116 BAX BAK1 DKOMoXVSpVv[3Srb36gRZN{[Xl?NXeyVGZvOy9zMDFOwG0>M1[xdlEzyqCqwrC=NF\tUVZFVVORMoLSbY5lfWOnczDhJIRwe2VvZHXw[Y5l\W62IHnuZ5Jm[XOnIHnuJGxEO0JvSVmgZ49vfmW{c3nvckBidmRiU2HTWG0yKGSnZ4Lh[IF1cW:wNGj5TXkzPTdzNUCyPC=>
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HCT116 BAX BAK1 DKOMorDSpVv[3Srb36gRZN{[Xl?MoO3NVAh|ryPM{SzeVEzyqCqwrC=MorUSG1UVw>?MojTbY5kemWjc3XzJGdHWC2OQ{PCJJB2dmO2YR?=MX:yOVcyPTB{OB?=
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HCT116 BAX BAK1 DKOMnroRZV1d3CqYXf5JGF{e2G7M3naflExKM7:TR?=M3jLdFEzyqCqwrC=M1HaNmROW09?M33NS4lv\HWlZYOgZUBkd22ybHX0[UBifXSxcHjh[4lkKHKnc4DvcpNmMl7VNlU4OTVyMki=
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U937 MX3BdI9xfG:|aYOgRZN{[Xl?NXXnfZY4OC53IN88US=>NVTmUXhqOjRiaB?=MoLB[Y5p[W6lZYOgZ4xm[X[jZ3Wgc4YhWEGUUDDhcoQh[2G|cHHz[U0{KGG|IIflcIwh[XNiTn;4ZUBt\X[nbB?=NH[1PJYzPTdzNECyOC=>
HL-60 AAA-Bcl-2NXLhPVJCSXCxcITvd4l{KEG|c3H5M4rrelAuPSEQvF2=NF\Rbm81QCCqMYDJR|UxRTBwOEeg{txu97zOaX7keYNmeyClZXzsJIFxd3C2b4Ppd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>Mn;KNlU4OTF2NkC=
HL-60 EEE-Bcl-2NWXvfFR1SXCxcITvd4l{KEG|c3H5M{XmUFAuPSEQvF2=NELQN2U1QCCqNVe0OpRtUUN3ME21JO69de,:jDDpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzNHHXc2kzPTdzMUS2NC=>
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K562/Mcl -1-IRESBimNHLid5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MXnJR|UxRTlwMzFOwG0>MmG5NlU2OzV7MEC=
K562/Bcl- 2-IRESBimM2nyNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MUjJR|UxRTBwM{Wg{txOM4TsXVI2PTN3OUCw
JurkatNVfZPItoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NXfKVpB[UUN3ME2wMlY3KM7:TR?=M{PUO|I2PTN3OUCw
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Kasumi-1NGqy[Y5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NVXzUHhiUUN3ME2wMlAyKM7:TR?=M33YWVI2PTN3OUCw
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... Click to View More Cell Line Experimental Data

In vivo In aggressive leukemia model, ABT-737 suppresses the leukemia burden by 53% at the 30 mg/kg, with significantly extended survival of mice. ABT-737 does not induce significantly abnormalities in blood cell counts or serum chemistries. [1] ABT-737 prolongs the survival of recipient mice transplanted with Bcl-2-transduced tumors. [2] ABT-737 shows great antitumor activity in an ATLL mouse model at a dose of 100 mg/kg. [5]
Features First-generation inhibitor of anti-apoptotic Bcl-2 proteins.

Protocol(Only for Reference)

Kinase Assay:

[1]

Fluorescence polarization assays Binding affinity of GST-Bcl-2 family proteins to the FITC-conjugated BH3 domain of Bim (FITC-Ahx-DMRPEIWIAQELRRIGDEFNAYYAR) is determined. Briefly, 100 nM of GST-Bcl-2 family fusion proteins are incubated with serial dilutions of ABT-737 in PBS for 2 min. Then, 20 nM of FITC-Bim BH3 peptide (FITC-Ahx-DMRPEIWIAQELRRIGDEFNAYYAR) is added. Fluorescence polarization is measured using an Analyst TM AD Assay Detection System after 10 min using the 96-well black plate. Then IC50 are determined.

Cell Assay:

[4]

Cell lines SCLC cell lines NCI-H889, NCI-H1963, NCI-H1417, NCI-H146, NCI-187, DMS79, NCI-1048, NCI-H82, NCI-H196, H69AR, and DMS114
Concentrations 0.001-10 μM
Incubation Time 48 hours
Method

SCLC cells are treated for 48 hours in 96-well tissue culture plates in a total volume of 100 μL tissue culture medium supplemented with 10% human serum. Viable cells are determined using the MTS assay.

Animal Study:

[1]

Animal Models Scid mice injected with Luc-expressing FD/ΔRaf-1:ER cells
Formulation 1 g/mL stock solution of ABT-737 in DMSO is added to a mixture of 30% propylene glycol, 5% Tween 80, 65% D5W (5% dextrose in water) (pH 4−5; final concentration of DMSO ≤ 1%)
Dosages 20 and 30 mg/kg
Administration For intraperitoneal (i.p.) every day

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Konopleva M, et al. Cancer Cell, 2006, 10(5), 375-388.

[2] van Delft MF,et al. Cancer Cell, 2006, 10(5), 389-399.

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Chemical Information

Download ABT-737 SDF
Molecular Weight (MW) 813.43
Formula

C42H45ClN6O5S2

CAS No. 852808-04-9
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 100 mg/mL (122.93 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 30% Propylene glycol, 5% Tween 80, 65% D5W 30mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name Benzamide, 4-[4-[(4'-chloro[1,1'-biphenyl]-2-yl)methyl]-1-piperazinyl]-N-[[4-[[(1R)-3-(dimethylamino)-1-[(phenylthio)methyl]propyl]amino]-3-nitrophenyl]sulfonyl]-

Frequently Asked Questions

  • Question 1
    What’s the recommended method about reconstitution of the compound for in vivo animal study?

    Answer: For oral administration, we suggest the vehicle: 30% Propylene glycol, 5% Tween 80, 65% D5W, at up to 30mg/ml; For injection, ABT-737 can be dissolved in 2% DMSO/50% PEG 300/5% Tween 80/ddH2O at 2.5 mg/ml.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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