ABT-737

Catalog No.S1002

Molecular Weight(MW): 813.43

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.

Cited by 144 Publications

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Purity & Quality Control

Choose Selective Bcl-2 Inhibitors

Biological Activity

Description

Features

First-generation inhibitor of anti-apoptotic Bcl-2 proteins.

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)
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 Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
OCI-Ly1	M2fuRmNmdGxiVnnhZoltcXS7IFHzd4F6	NXXMRZBnOjVyIH7NxsA>	M{fnNlczKGh?	MnH2SG1UVw>?	MmOzZ4F2e2WmIEm3KUBtd3O\|IH;mJJZq[WKrbHn0fUBqdiClZXzsd{B1emGwc3\lZ5Rm\CC5aYToJGJEVDZic3nSUmE>	NUjtb2N3OjZ4NUeyPFg>
KG1a	NVfyOmRvS2WubDDWbYFjcWyrdImgRZN{[Xl?	NIKwcY8xNTFyIN88US=>	MYCyOEBp	M3;pNWROW09?	M33kOmlEPTB;Nz62PEDPxE1uIHTlZ5Jm[XOnczDj[YxtKH[rYXLpcIl1gSCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>?	M3fTNVI3PTV{N{Gy
Kasumi-1	Ml20R4VtdCCYaXHibYxqfHliQYPzZZk>	NVzWeJJmOC1zMDFOwG0>	NUm5fYpXOjRiaB?=	MW\EUXNQ	NVXKdJlnUUN3ME20Mlg4KM7:TTyg[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:\|ZT3k[ZBmdmSnboSgcYFvdmW{	NILPcWIzPjV3MkexNi=>
KG1a	M{TNcGFxd3C2b4Ppd{BCe3OjeR?=	M3KwW\|AuOTBizszN	MX:yOEBp	Mm\4SG1UVw>?	M{ew[Ilv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?	MkLuNlY2PTJ5MUK=
Kasumi-1	M1;yUmFxd3C2b4Ppd{BCe3OjeR?=	M3nNW\|AuOTBizszN	NVOxU5NPOjRiaB?=	NXT6dXF[TE2VTx?=	MnHZbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>?	NFfSd48zPjV3MkexNi=>
MC-3	M2PUU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NYXtUmpCPS9zMD:yNEDPxE1?	MomyNlQhcA>?	NIPqN45FVVOR	NVvLV5A3cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?	NH;Lbo4zPjR2N{[xOS=>
HN22	M{LtO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NF;RSZczNjVxNz61M\|IzNjVizszN	M3vwUFI1KGh?	MYnEUXNQ	MVfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>	MkOzNlY1PDd4MUW=
MC-3	NYXwWWtKSXCxcITvd4l{KEG\|c3H5	NHGzPWQ2NzFyL{KwJO69VQ>?	NGr6[4czPCCq	NEfmOlFFVVOR	MnnKbY5lfWOnczDjZZNx[XOnLX3l[IlifGWmIHHwc5B1d3Orcx?=	NEfoSXUzPjR2N{[xOS=>
HN22	NWTzXnlpSXCxcITvd4l{KEG\|c3H5	NXz6Z3lvOi53L{euOU8zOi53IN88US=>	MnPrNlQhcA>?	MW\EUXNQ	MVnpcoR2[2W\|IHPhd5Bie2VvbXXkbYF1\WRiYYDvdJRwe2m\|	M4HPVlI3PDR5NkG1
MOLT-4	NU\ZU\|RST3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NGXZU5cyOC13MECwJI5O	MXm3NkBp	M37YXWROW09?	MkPFTWM2OD1yLkG5PEDPxE1?	M3uzR\|I3Ozl{M{Oy
RS4;11	M3\1cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NVW3b4Q{OTBvNUCwNEBvVQ>?	NYjuTGxOPzJiaB?=	MmjnSG1UVw>?	MVHJR\|UxRTBwMECyJO69VQ>?	M{j5OVI3Ozl{M{Oy
JURKAT	MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MX[xNE02ODByIH7N	MmDFO\|IhcA>?	NX7XU5l2TE2VTx?=	MX7JR\|UxRTZ4IN88US=>	MnHFNlY{QTJ\|M{K=
CEM R	M120cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Mn30NVAuPTByMDDuUS=>	MWK3NkBp	NXHvVIhTTE2VTx?=	MXPJR\|UxRTVwNDFOwG0>	MUCyOlM6OjN\|Mh?=
CEM S	MlewS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MnvBNVAuPTByMDDuUS=>	MYC3NkBp	NU\POnZ7TE2VTx?=	M1;RUmlEPTB;MUKuNUDPxE1?	NEm1SZYzPjN7MkOzNi=>
MOLT-4	NEnMdotCeG:ydH;zbZMhSXO\|YYm=	MmXYNVAuOTByMDDuUS=>	MkfqNlQhcA>?	NWPQUXNKTE2VTx?=	MYTjZZV{\XNidHjlJINt\WG4YXflJI9nKEKlbD2yJIFv\CC2aHWg[I94dnKnZ4XsZZRqd25ib3[gRoNtNXiOIHHu[EBO[2xvMR?=	MWCyOlM6OjN\|Mh?=
CEM S	MUjBdI9xfG:\|aYOgRZN{[Xl?	NIXqW\|EyOC1zMECwJI5O	NY\JV4NDOjRiaB?=	NWjoe3AzTE2VTx?=	MXnjZZV{\XNidHjlJINt\WG4YXflJI9nKEKlbD2yJIFv\CC2aHWg[I94dnKnZ4XsZZRqd25ib3[gRoNtNXiOIHHu[EBO[2xvMR?=	MlfQNlY{QTJ\|M{K=
JURKAT	MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NWjjNoxpOTByLUGwNFAhdk1?	MUe0PEBp	M{TmUWROW09?	NGjHToRKSzVyPUm1OeKyQS5\|IH7N	NIP5c3kzPjF5MkK2PS=>
LOUCY	NGX1R2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NYGzUGlWOTByLUGwNFAhdk1?	NIH4[Ho1QCCq	MlzISG1UVw>?	M1TtUGlEPTB;M{KuPOKyOTBwOTDuUS=>	MUeyOlE4OjJ4OR?=
WM-115	M3LlRWNmdGxiVnnhZoltcXS7IFHzd4F6	NVPIVmVYOTBywrDuUS=>	MnLuO\|IhcA>?		NX:5cIk2\W6qYX7j[ZMh[3W{Y4XtbY4ucW6mdXPl[EBidnSrLYP1dpZqfmGuwrC=	NGjsWmUzPjFzNke3Oi=>
B16	NGezToFE\WyuIG\pZYJqdGm2eTDBd5NigQ>?	MnqzNVAxyqCwTR?=	NFq0bYs4OiCq		MXnlcohidmOnczDjeZJkfW2rbj3pcoR2[2WmIHHueIkue3W{dnn2ZYzDqA>?	M1TMSFI3OTF4N{e2
HL-60	NITkVYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		Ml\JO\|IhcA>?		NHfzOZVKSzVywrC9JFExNjdibl2=	M3;HcFI3ODR3NkC5
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HCT116	NIXycIRHfW6ldHnvckBCe3OjeR?=	M4jMXFMwOTBizszN	NFvRW44yOsLiaNMg	MXfEUXNQ	M2TR[Ilv\HWlZYOgZUBld3OnLXTldIVv\GWwdDDpcoNz\WG\|ZTDpckBNSzOELVnJJINwdn[ncoPpc44h[W6mIGPRV3ROOSCmZXfyZYRifGmxbh?=	NX;kXYZsOjV5MUWwNlg>
HCT116 BAX BAK1 DKO	M4LaemZ2dmO2aX;uJGF{e2G7	NHvYOZY{NzFyIN88US=>	MnW4NVLDqGkEoB?=	MlnjSG1UVw>?	M2HYS4lv\HWlZYOgZUBld3OnLXTldIVv\GWwdDDpcoNz\WG\|ZTDpckBNSzOELVnJJINwdn[ncoPpc44h[W6mIGPRV3ROOSCmZXfyZYRifGmxbh?=	NULOUZV7OjV5MUWwNlg>
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HL-60 AAA-Bcl-2	MnuwRZBweHSxc3nzJGF{e2G7	NHzZO2UxNTVizszN	NXnPbJdbPDhiaB?=		M37iTmlEPTB;MD64O{DPxG4xvJzpcoR2[2W\|IHPlcIwh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz	MUeyOVcyOTR4MB?=
HL-60 EEE-Bcl-2	NWf3WFFJSXCxcITvd4l{KEG\|c3H5	MXywMVUh\|ryP	NV7qXlk4PDhiaB?=		NXL0UGp1UUN3ME21JO69de,:jDDpcoR2[2W\|IHPlcIwh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz	MnPGNlU4OTF2NkC=
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K562	M1jZemNmdGxiVnnhZoltcXS7IFHzd4F6	M3rxb\|EuOTBizszN	NVr1XZBHPDhiaB?=	MmHJSG1UVw>?	MnjwTWM2OD1{Nj63JO69VQ>?	M1XyTVI2PTl4NU[x
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Jurkat	MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MWHJR\|UxRTBwNk[g{txO	M3LLSVI2PTN3OUCw
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C1498	MkfmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NIG4XWVKSzVyPU[uNVMh\|ryP	NELKU5czPTV\|NUmwNC=>
RPMI 8226	MlnES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				Mn:wTWM2OD1yLkK1JO69VQ>?	MmHTNlU2OzV7MEC=
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Caco-2	MV\D[YxtKF[rYXLpcIl1gSCDc4PhfS=>	Mn3YNE0yOCEQvF2=	MlrBNlTjiImqwrC=	NE\n[lBFVVOR	NIjsNllKSzVyPUG5MlfjiIoEtV2=	NY\rfnFJOjV\|MESzPFM>
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HaCaT	NIrXdmhHfW6ldHnvckBCe3OjeR?=	MojKNVDjiIoQvF2=	NWC3bVJqOjRxNEigbC=>	MXjEUXNQ	MnXhbY5lfWOnczDNUXAh[W6mIFTORUBnemGpbXXueIF1cW:w	NFfIW2UzPTJzMEe5OS=>
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U266	NGKzeG9HfW6ldHnvckBCe3OjeR?=	MWO1NFAwPzVyIH7N	MVKyOE81QCCq	MW\EUXNQ	MnPs[I94dnKnZ4XsZZRmeyCEaX2sJJBzcW6laYDhcIx6KHSqZTDFUEBqe2:ob4Lt	MY[yOVIxQDh6OB?=
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CX-1	NUfmOJlWT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NVPzXGZLOC5{4pETOlAh\|ryP	NGjtXG84OiCq	MUPEUXNQ	MWLJR\|UxRTFwODFOwG0>	NGe1XoEzPTJyOEi4Ni=>
LS174T	NXzJUIExT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NUfkPJl3OC5{4pETOlAh\|ryP	MorGO\|IhcA>?	MmLRSG1UVw>?	NYrwVphJUUN3ME2xPE4{KM7:TR?=	NHnwU\|UzPTJyOEi4Ni=>
HT29	M3;Pd2Fxd3C2b4Ppd{BCe3OjeR?=	NHK1V\|AyNzVxMUCg{txO	MUK0PEBp		Mnj3Z4F2e2W\|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK=	NHi5VZEzPTF7MkG4PC=>
SW480	NEXwSodCeG:ydH;zbZMhSXO\|YYm=	MVqxM\|UwOTBizszN	MnrjOFghcA>?		NHvYV21k[XW\|ZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>	MnvRNlUyQTJzOEi=
Colo205	NFzJWmVCeG:ydH;zbZMhSXO\|YYm=	MW[xM\|UwOTBizszN	NYezfnVWPDhiaB?=		MYHjZZV{\XNiY3XscEBl\WG2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?=	MVSyOVE6OjF6OB?=
Caco2	NGnvellCeG:ydH;zbZMhSXO\|YYm=	MkfwNU82NzFyIN88US=>	NE\sSJU1QCCq		NIX0[Hhk[XW\|ZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>	NFHPTlMzPTF7MkG4PC=>
PCI-13	M373eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NE\Nd3Q4OiCq	NG\vWI1FVVOR	NIfIUJdIUTVyPUG1JOKyKDFwODFOwG0>	MUWyOVE{QTN6Nx?=
PCI-15B	Mom5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		Mn\4O\|IhcA>?	NF;vPVZFVVOR	NWm1PFA5T0l3ME2xNUDDuSB2LkWg{txO	MYqyOVE{QTN6Nx?=
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UM-SCC47	M3XLVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		M3fuT\|czKGh?	MWTEUXNQ	MYfHTVUxRTF7INMxJFEzNjNizszN	MX6yOVE{QTN6Nx?=
93-VU-147T	NVnsPXNLT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		Mn[yO\|IhcA>?	MkLkSG1UVw>?	MlPUS2k2OD12LkOgxtEhOy53IN88US=>	NH;jOWozPTF\|OUO4Oy=>
UD-SCC2	M1;JV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		M3zNUVczKGh?	NF3Wd\|lFVVOR	NYK2TndST0l3ME2yPEDDuSB{Lkmg{txO	NWTGOo5POjVzM{mzPFc>
UPCI:SCC90	M1rMRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NXXZdGJjPzJiaB?=	MWjEUXNQ	NUT0c2h5T0l3ME22MlYhyrFiMT61JO69VQ>?	NFnGU28zPTF\|OUO4Oy=>
RPMI-8226	NF[4NVlE\WyuIG\pZYJqdGm2eTDBd5NigQ>?	NXPUUVZ6OTJ3L{K1NE82ODBibl2=	MXW0PIjDqA>?	MkPFSG1UVw>?	NV;jVoFN\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy	NVT4NWJ4OjVyMEiyNFI>
OPM-2	NVjGTpZ4S2WubDDWbYFjcWyrdImgRZN{[Xl?	NUTXZYRCOTJ3L{K1NE82ODBibl2=	MmL4OFhpyqB?	MnfaSG1UVw>?	Mn7P[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:\|ZT3k[ZBmdmSnboSgcYFvdmW{	NH:ze5AzPTByOEKwNi=>
RPMI-8226	NV;2OYFRSXCxcITvd4l{KEG\|c3H5	MV6xNlUwOjVyL{WwNEBvVQ>?	MnfhOFhpyqB?	M{DENGROW09?	M{n1Uolv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?	MlPkNlUxODh{MEK=
OPM-2	MWTBdI9xfG:\|aYOgRZN{[Xl?	MUexNlUwOjVyL{WwNEBvVQ>?	NUWxc5RxPDiqwrC=	NXPTS\|dRTE2VTx?=	MWLpcoR2[2W\|IHPlcIwh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz	Mmr0NlUxODh{MEK=
COG-LL-319	M3LIOGZ2dmO2aX;uJGF{e2G7	M3fLdFExOCCwTR?=	Mkf6NU8{NzZiaB?=	NFq3[o5FVVOR	MVPpcoR2[2W\|IHPhd5Bie2VvZHXw[Y5l\W62IF3jcE0yKGOuZXH2ZYdm	MkD0NlQ6PTF2N{K=
RS4;11	NV6yU2pKTnWwY4Tpc44hSXO\|YYm=	M1OzSlExOCCwTR?=	Ml3vNU8{NzZiaB?=	NYO3THVQTE2VTx?=	M3rWVolv\HWlZYOgZ4F{eGG\|ZT3k[ZBmdmSnboSgUYNtNTFiY3zlZZZi\2V?	NFnic2ozPDl3MUS3Ni=>

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	PARP / c-PARP / cleaved caspase 3 ; PubMed: 21393866 J Clin Invest H146 cells were preincubated in normoxia or hypoxia (1% O2) for 18 hours prior to treatment with ABT-737 (89.1 nM ), after which cells were harvested for protein analysis by Western blot. Hif-1a; PubMed: 22006676 Mol Cancer Ther Representative western blots for HIF-1α, PARP and cleaved caspase 3 in response to 24-72 hr exposure to ABT-737 in varying concentration in normoxia and hypoxia in 4 neuroblastoma cell lines. Actin is shown as a loading control. Blots are representative of 3 independent experiments. γ-H2AX / p-ATM; PubMed: 21084274 Cancer Res Induction of γ-H2AX and p-ATM by ABT-737. Cells were treated with 10 µmol/L ABT-737 for 24 hours and then maintained in fresh media for 1 or 2 more days prior to Western blot analysis.	21393866 22006676 21084274
Immunofluorescence	cytochrome C; PubMed: 26447615 Oncotarget Immunocytochemistry revealed the release of mitochondrial cytochrome c (green) into the cytoplasm after ABT-737 exposure (20 μM in MC-3 cells and 22.5 μM in HN22 cells) for 24 hr. MitoTracker (red) staining labels mitochondria within each field. Bax; PubMed: 26447615 Oncotarget Immunocytochemistry revealed the mitochondrial translocation of Bax from the cytoplasm after ABT-737 treatment (20 μM in MC-3 cells and 22.5 μM in HN22 cells) for 24 hr. MitoTracker (red) staining labels mitochondria within each field C. To assess whether ABT-737 treatment has an effect on the dimerization of Bax, the levels of dimeric Bax were measured with or without ABT-737 treatment in MC-3 and HN22 cells. Bim; PubMed: 26447615 Oncotarget Immunocytochemistry revealed the mitochondrial translocation of Bim from the cytoplasm after ABT-737 treatment (20 μM in MC-3 cells and 22.5 μM in HN22 cells) for 24 hr. MitoTracker (red) staining labels mitochondria within each field. AIF; PubMed: 25034785 Cell Death Differ localization of apoptosis inducing factor (AIF) in LCSC pre-stained with Mitotracker Red and untreated or treated with 500 nM ABT-737 for 48 h. Magnification × 60, zoom × 3, bar 20 μm. p65 ; PubMed: 28846096 Nat Cell Biol BCL-xL dependent SVEC cells were treated with ABT-737 (10 μM) +/- Q-VD-Oph (30 μM) for 1 h, immunostained for p65 and analysed by confocal microscopy. TNF (20 ng/ml) was used as positive control for p65 nuclear translocation. Scale bar represents 30μM. Representative images from three independent experiments.	26447615 25034785 28846096
Growth inhibition assay	Cell viability; PubMed: 22311987 J Biol Chem Stably transfected K562 cells were treated with increasing concentrations of ABT-737, obatoclax, or maritoclax for 24 h. Cell viability was determined by measuring intracellular ATP levels with the CellTiter Glo assay.	22311987
ELISA	IL-6 / IL-8; PubMed: 21084274 Cancer Res The secretion of IL-6 and IL-8 in PV-10 cells treated with DMSO, ABT-737 or enantiomer for 24 hours was determined by ELISA.	21084274

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]

Protocol

Kinase Assay: ^[1]	+ Expand 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 Research: ^[4]	+ Expand 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. (Only for Reference)
Animal Research: ^[1]	+ Expand 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 (Only for Reference)

References

+ Expand

Solubility (25°C)

In vitro	DMSO	100 mg/mL (122.93 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 30% Propylene glycol, 5% Tween 80, 65% D5W For best results, use promptly after mixing.	30mg/mL

* 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 Information Download ABT-737 SDF

Molecular Weight	813.43
Formula	C₄₂H₄₅ClN₆O₅S₂
CAS No.	852808-04-9
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	N/A

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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.

Handling Instructions

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

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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.

Bcl-2 Signaling Pathway Map

Bcl-2 Inhibitors with Unique Features

Selective Bcl-2 Inhibitor

ABT-199 (GDC-0199) : Bcl-2-selective, K_i<0.01 nM.
Most Potent Bcl-2 Inhibitor

ABT-263 (Navitoclax) : Bcl-xL, K_i≤ 0.5 nM; Bcl-2, K_i≤ 1 nM; Bcl-w, K_i≤ 1 nM.
Bcl-2 Inhibitor in Clinical Trial

Obatoclax Mesylate (GX15-070) : Phase II for leukemia, lymphoma, myelofibrosis, and mastocytosis.
Newest Bcl-2 Family Activator

BAM7 : Direct and selective activator of proapoptotic Bax with EC50 of 3.3 μM.

Related Bcl-2 Products

A-1210477 ^New

A-1210477 is a potent and selective MCL-1 inhibitor with K_i and IC50 of 0.454 nM and 26.2 nM, respectively, >100-fold selectivity over other Bcl-2 family members.
MI-773 (SAR405838) ^New

MI-773 (SAR405838) is an orally available MDM2 antagonist with K_i of 0.88 nM. Phase 1.
Navitoclax (ABT-263)

Navitoclax (ABT-263) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with K_i of ≤ 0.5 nM, ≤1 nM and ≤1 nM in cell-free assays, but binds more weakly to Mcl-1 and A1. Phase 2.
Venetoclax (ABT-199, GDC-0199)

Venetoclax (ABT-199, GDC-0199) is a Bcl-2-selective inhibitor with K_i 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.

Features:Re-engineered version of ABT-263 (Navitoclax).
UMI-77

UMI-77 is a selective Mcl-1 inhibitor with Ki of 490 nM, showing selectivity over other members of Bcl-2 family.
Obatoclax Mesylate (GX15-070)

Obatoclax Mesylate (GX15-070) is an antagonist of Bcl-2 with K_i of 0.22 μM in a cell-free assay, can assist in overcoming MCL-1 mediated resistance to apoptosis. Phase 3.

Features:Potential 1st-in-class small molecule antagonist of Bcl-2 designed to inhibit all relevant Bcl-2 family members, including Mcl-1.
TW-37

TW-37 is a novel nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with K_i of 0.29 μM, 1.11 μM and 0.26 μM in cell-free assays, respectively.
Sabutoclax

Sabutoclax(BI-97C1) is a pan-Bcl-2 inhibitor, including Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively.
AT101

AT101, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with K_i of 0.32 μM, 0.48 μM and 0.18 μM in cell-free assays; does not inhibit BIR3 domain and BID. Phase 2.

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ABT-737

Cited by 144 Publications

Purity & Quality Control

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Biological Activity

Protocol

References

Solubility (25°C)

Chemical Information Download ABT-737 SDF

Bio Calculators

Molarity Calculator

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

Dilution Calculator

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

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Total Molecular Weight: g/mol

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molarity Calculator

Tech Support

Frequently Asked Questions

Bcl-2 Signaling Pathway Map

Bcl-2 Inhibitors with Unique Features

Related Bcl-2 Products

Choose Your Country or Region

By Signaling Pathways

By product type

ABT-737

Cited by 144 Publications

Purity & Quality Control

Choose Selective Bcl-2 Inhibitors

Biological Activity

Protocol

References

Solubility (25°C)

Chemical Information Download ABT-737 SDF

Bio Calculators

Molarity Calculator

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

Dilution Calculator

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

The Serial Dilution Calculator Equation

Serial Dilutions

Computed Result

Molecular Weight Calculator

Total Molecular Weight: g/mol

Instructions to calculate molar mass (molecular weight) of a chemical compound:

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molarity Calculator

Tech Support

Frequently Asked Questions

Bcl-2 Signaling Pathway Map

Bcl-2 Inhibitors with Unique Features

Related Bcl-2 Products

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)