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ABT-737

Name: ABT-737
Brand: Selleck Chemicals
SKU: S1002
Rating: 5 (322 reviews)

Catalog No.S1002

For research use only.

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. ABT-737 induces mitochondrial pathway apoptosis and mitophagy. Phase 2.

CAS No. 852808-04-9

Selleck's ABT-737 has been cited by 322 publications

Purity & Quality Control

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Bcl-2 Signaling Pathway Map

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	NITzcWhE\WyuIG\pZYJqdGm2eTDBd5NigQ>?	M{fxOFI2OCCwTdMg	NVHQPGFsPzJiaB?=	MonISG1UVw>?	M17seINifXOnZDC5O{UhdG:\|czDv[kB3cWGkaXzpeJkhcW5iY3XscJMhfHKjboPm[YN1\WRid3n0bEBDS0x4IIPpVm5C	NFLn[Ho9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[1O\|I5QCd-Mk[2OVczQDh:L3G+
KG1a	MWTD[YxtKF[rYXLpcIl1gSCDc4PhfS=>	NGeyVZIxNTFyIN88US=>	NXLRdlhJOjRiaB?=	M2O3PWROW09?	NVznTXJFUUN3ME23MlY5KM7:TTyg[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:\|ZT3k[ZBmdmSnboSgcYFvdmW{	M{K4dFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NUWyO\|EzLz5{NkW1NlcyOjxxYU6=
Kasumi-1	MmXPR4VtdCCYaXHibYxqfHliQYPzZZk>	M4q2UlAuOTBizszN	M17p[\|I1KGh?	NIHEXWJFVVOR	NWPBUGM5UUN3ME20Mlg4KM7:TTyg[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:\|ZT3k[ZBmdmSnboSgcYFvdmW{	MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV3MkexNkc,OjZ3NUK3NVI9N2F-
KG1a	NWHNeGxOSXCxcITvd4l{KEG\|c3H5	MX:wMVExKM7:TR?=	NWr4NJBMOjRiaB?=	Ml35SG1UVw>?	NV3BNHdlcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?=	MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV3MkexNkc,OjZ3NUK3NVI9N2F-
Kasumi-1	NE\lSpFCeG:ydH;zbZMhSXO\|YYm=	M1fpcVAuOTBizszN	NV3XNmhXOjRiaB?=	M4G2RmROW09?	MnHEbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>?	Ml;BQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3NUK3NVIoRjJ4NUWyO\|EzRC:jPh?=
MC-3	MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NF7FZZg2NzFyL{KwJO69VQ>?	MYeyOEBp	MlH3SG1UVw>?	M3\nXIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz	MmDUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ2NEe2NVUoRjJ4NES3OlE2RC:jPh?=
HN22	NFjCSXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NFnNfmIzNjVxNz61M\|IzNjVizszN	NY\vcplbOjRiaB?=	Mo[2SG1UVw>?	M4j3RolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz	M2fZ[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NES3OlE2Lz5{NkS0O\|YyPTxxYU6=
MC-3	MmPCRZBweHSxc3nzJGF{e2G7	NHe5fpY2NzFyL{KwJO69VQ>?	M4rGeFI1KGh?	MmX1SG1UVw>?	MlW3bY5lfWOnczDjZZNx[XOnLX3l[IlifGWmIHHwc5B1d3Orcx?=	MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjR2N{[xOUc,OjZ2NEe2NVU9N2F-
HN22	M{LIXWFxd3C2b4Ppd{BCe3OjeR?=	MWSyMlUwPy53L{KyMlUh\|ryP	M2i0flI1KGh?	MnXESG1UVw>?	NV61SpJUcW6mdXPld{Bk[XOyYYPlMY1m\GmjdHXkJIFxd3C2b4Ppdy=>	MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjR2N{[xOUc,OjZ2NEe2NVU9N2F-
MOLT-4	MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MWixNE02ODByIH7N	MnzOO\|IhcA>?	MoXWSG1UVw>?	MYfJR\|UxRTBwMUm4JO69VQ>?	Mor4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ\|OUKzN\|IoRjJ4M{myN\|MzRC:jPh?=
RS4;11	NYfHT5llT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NGH4WmEyOC13MECwJI5O	NWjlcpUzPzJiaB?=	MnrNSG1UVw>?	MXPJR\|UxRTBwMECyJO69VQ>?	NWnGfGpGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[zPVI{OzJpPkK2N\|kzOzN{PD;hQi=>
JURKAT	MmOxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MYCxNE02ODByIH7N	NUDNOY1sPzJiaB?=	NI\qOHFFVVOR	M3PFeGlEPTB;Nk[g{txO	M4f2cFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{myN\|MzLz5{NkO5NlM{OjxxYU6=
CEM R	NXfidVBNT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MVSxNE02ODByIH7N	NFL0W5E4OiCq	MUTEUXNQ	MXPJR\|UxRTVwNDFOwG0>	M1j1VlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{myN\|MzLz5{NkO5NlM{OjxxYU6=
CEM S	MmHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M{Hoe\|ExNTVyMECgcm0>	NUHa[ldnPzJiaB?=	NIPi[m9FVVOR	M3TUV2lEPTB;MUKuNUDPxE1?	M4HZXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{myN\|MzLz5{NkO5NlM{OjxxYU6=
MOLT-4	NELCbmZCeG:ydH;zbZMhSXO\|YYm=	MYixNE0yODByIH7N	NED5NpEzPCCq	MkL4SG1UVw>?	MX;jZZV{\XNidHjlJINt\WG4YXflJI9nKEKlbD2yJIFv\CC2aHWg[I94dnKnZ4XsZZRqd25ib3[gRoNtNXiOIHHu[EBO[2xvMR?=	MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN7MkOzNkc,OjZ\|OUKzN\|I9N2F-
CEM S	MXzBdI9xfG:\|aYOgRZN{[Xl?	MV:xNE0yODByIH7N	MUKyOEBp	NVXuOZdYTE2VTx?=	MX;jZZV{\XNidHjlJINt\WG4YXflJI9nKEKlbD2yJIFv\CC2aHWg[I94dnKnZ4XsZZRqd25ib3[gRoNtNXiOIHHu[EBO[2xvMR?=	MonBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ\|OUKzN\|IoRjJ4M{myN\|MzRC:jPh?=
JURKAT	NIjaR3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MYWxNFAuOTByMDDuUS=>	MWO0PEBp	NUfxUIdNTE2VTx?=	M4DNcGlEPTB;OUW1xtE6NjNibl2=	MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjF5MkK2PUc,OjZzN{KyOlk9N2F-
LOUCY	MlWzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NXXXRphYOTByLUGwNFAhdk1?	NV[yZlJMPDhiaB?=	NULPOpFETE2VTx?=	MnnNTWM2OD1\|Mj64xtEyOC57IH7N	NEn1SYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkG3NlI3QSd-Mk[xO\|IzPjl:L3G+
WM-115	MnfDR4VtdCCYaXHibYxqfHliQYPzZZk>	NITCT2QyODEEoH7N	MkLyO\|IhcA>?		NHjSO5JmdmijbnPld{BkfXKldX3pck1qdmS3Y3XkJIFvfGlvc4Xyeol3[W{EoB?=	MoflQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzMU[3O\|YoRjJ4MUG2O\|c3RC:jPh?=
B16	NUj3Z\|ZNS2WubDDWbYFjcWyrdImgRZN{[Xl?	MVSxNFDDqG6P	Mn3WO\|IhcA>?		NEPreFVmdmijbnPld{BkfXKldX3pck1qdmS3Y3XkJIFvfGlvc4Xyeol3[W{EoB?=	NIfCSmw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGxOlc4Pid-Mk[xNVY4PzZ:L3G+
HL-60	M1HkPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MYq3NkBp		M{\KdmlEPTEEoE2gNVAvPyCwTR?=	NUGzeppIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wOFU3ODlpPkK2NFQ2PjB7PD;hQi=>
MOLM-13	Mm\CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		M{LZSFczKGh?		MkK3TWM2OMLiPTCyO{46KG6P	NFjQUVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC0OVYxQSd-Mk[wOFU3ODl:L3G+
OCI-AML3	Mnf6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NGHjdJk4OiCq		MYXJR\|UxyqB;IEG5OVAhdk1?	NITaVmQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC0OVYxQSd-Mk[wOFU3ODl:L3G+
BCWM.1	M1nrWmFxd3C2b4Ppd{BCe3OjeR?=	MoPGNE0yNjZizszN	MlTzNlQhcA>?		NGD2e2xqdmS3Y3XzJINmdGxiYYDvdJRwe2m\|	MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh7M{K5NEc,OjV6OUOyPVA9N2F-
MWCL-1	M1\TdWFxd3C2b4Ppd{BCe3OjeR?=	Mn\CNE0yNjZizszN	M1XLZ\|I1KGh?		MXzpcoR2[2W\|IHPlcIwh[XCxcITvd4l{	M1vqUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEmzNlkxLz5{NUi5N\|I6ODxxYU6=
MM.1s	NHPyNVdCeG:ydH;zbZMhSXO\|YYm=	NWjLfI95OC1zLk[g{txO	MmrLNlQhcA>?		MofXbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>?	M4TG[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEmzNlkxLz5{NUi5N\|I6ODxxYU6=
HCT116	MYjGeY5kfGmxbjDBd5NigQ>?	NWjmc3FNOy9zMDFOwG0>	MXSxNuKhcMLi	M2L6VWROW09?	MVzpcoR2[2W\|IHGg[I9{\S2mZYDlcoRmdnRiaX7jdoVie2ViaX6gUGM{Si2LSTDjc453\XK\|aX;uJIFv\CCVUWPUUVEh\GWpcnHkZZRqd25?	NF[0Tmw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUexOVAzQCd-MkW3NVUxOjh:L3G+
HCT116 BAX BAK1 DKO	M4fYbWZ2dmO2aX;uJGF{e2G7	MmTpN{8yOCEQvF2=	MVexNuKhcMLi	NIPQSHpFVVOR	NYntblE4cW6mdXPld{BiKGSxc3Wt[IVx\W6mZX70JIlv[3KnYYPlJIlvKEyFM1KtTWkh[2:wdnXyd4lwdiCjbnSgV3FUXE1zIHTl[5Ji\GG2aX;u	M3fJd\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{G1NFI5Lz5{NUexOVAzQDxxYU6=
HCT116	M4j2[WZ2dmO2aX;uJGF{e2G7	NFfJXGkyOCEQvF2=	MnG0NVLDqGkEoB?=	M4fUZWROW09?	NX\Ne5JJcW6lcnXhd4V{KEeIUD3MR\|NDKHC3bnP0ZS=>	NX\yZo9GRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3NVUxOjhpPkK1O\|E2ODJ6PD;hQi=>
HCT116 BAX BAK1 DKO	NHXVfYNHfW6ldHnvckBCe3OjeR?=	M37wWlExKM7:TR?=	MkTNNVLDqGkEoB?=	MU\EUXNQ	M2rHcYlv[3KnYYPld{BITlBvTFOzRkBxfW6ldHG=	MofsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5MUWwNlgoRjJ3N{G1NFI5RC:jPh?=
HCT116	M1;kO2F2fG:yaHHnfUBCe3OjeR?=	NWPCfVRZOTBizszN	MUexNuKhcMLi	M1za[mROW09?	NWHVcnI1cW6mdXPld{BiKGOxbYDs[ZRmKGG3dH;wbIFocWNicnXzdI9ve2V?	NGjubGQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUexOVAzQCd-MkW3NVUxOjh:L3G+
HCT116 BAX BAK1 DKO	M4jPUGF2fG:yaHHnfUBCe3OjeR?=	M3LwS\|ExKM7:TR?=	MW[xNuKhcMLi	MYDEUXNQ	MYTpcoR2[2W\|IHGgZ49ueGyndHWgZZV1d3CqYXfpZ{Bz\XOyb37z[S=>	MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTdzNUCyPEc,OjV5MUWwNlg9N2F-
U937	MWDBdI9xfG:\|aYOgRZN{[Xl?	MV:wMlEzPS1{IN88US=>	NX\F[ZpROjRiaB?=		MXrlcohidmOnczDETGEwYC1zMT3pcoR2[2WmIHHwc5B1d3Orcx?=	MljuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5MUSwNlQoRjJ3N{G0NFI1RC:jPh?=
U937	NWW4bolvSXCxcITvd4l{KEG\|c3H5	MlvsNE42KM7:TR?=	MmjJNlQhcA>?		M2XyW4VvcGGwY3XzJINt\WG4YXflJI9nKFCDUmCgZY5lKGOjc4Dhd4UuOyCjczD3[YxtKGG\|IF7vfIEhdGW4ZXy=	MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTdzNECyOEc,OjV5MUSwNlQ9N2F-
HL-60 AAA-Bcl-2	NX\DPWZlSXCxcITvd4l{KEG\|c3H5	NFnEUIQxNTVizszN	MX20PEBp		MofQTWM2OD1yLki3JO69de,:jHnu[JVk\XNiY3XscEBieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI>	NYHI[2NuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3NVE1PjBpPkK1O\|EyPDZyPD;hQi=>
HL-60 EEE-Bcl-2	NWDsV5h2SXCxcITvd4l{KEG\|c3H5	NHH0OHExNTVizszN	NHH6Rno1QCCq		MmG4TWM2OD13IN88cg+9lCCrbnT1Z4V{KGOnbHygZZBweHSxc3nzJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy	Ml;QQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5MUG0OlAoRjJ3N{GxOFYxRC:jPh?=
U87	NWjSVmZtTnWwY4Tpc44hSXO\|YYm=	NXKw[29WPTBizszN	NHrMOnczPCCq		M1zNeZJm\HWlZYOgeIhmKG2UTlGg[ZhxemW\|c3nvckBt\X[nbIOgc4YhVU2SLUKsJG1OWC1zNDDhcoQhSmOuLUK=	M4Hw[\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Nk[3OlY{Lz5{NU[2O\|Y3OzxxYU6=
K562	M1HNRWNmdGxiVnnhZoltcXS7IFHzd4F6	MUexMVExKM7:TR?=	Ml;IOFghcA>?	M2X3O2ROW09?	NEjmfnVKSzVyPUK2Mlch\|ryP	NHS4WJA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUW5OlU3OSd-MkW1PVY2PjF:L3G+
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MM.1S	M3;FbmZ2dmO2aX;uJGF{e2G7	NH;XcWE2ODBxN{WwJI5O	NF30PI8zPC92ODDo	MoftSG1UVw>?	Mle1[I94dnKnZ4XsZZRmeyCEaX2sJJBzcW6laYDhcIx6KHSqZTDFUEBqe2:ob4Lt	M1rVTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkC4PFg5Lz5{NUKwPFg5QDxxYU6=
Clone A	NVj0Ro1[T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M1Swb\|AvOuLCk{[wJO69VQ>?	MoOyO\|IhcA>?	M{Plc2ROW09?	M1qyO2lEPTB;Nz61JO69VQ>?	NYntOIFiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNFg5QDJpPkK1NlA5QDh{PD;hQi=>
CX-1	NUnxeoZLT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NWn0T4ZFOC5{4pETOlAh\|ryP	NVK3OnJyPzJiaB?=	M1K0N2ROW09?	NWfyNWk2UUN3ME2xMlgh\|ryP	NHrUN2Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKwPFg5Oid-MkWyNFg5QDJ:L3G+
LS174T	NFnXZYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NFXRUWUxNjMkgKO2NEDPxE1?	Ml3CO\|IhcA>?	MkHLSG1UVw>?	NHryZpVKSzVyPUG4MlMh\|ryP	NXrBXG9IRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNFg5QDJpPkK1NlA5QDh{PD;hQi=>
HT29	NY\wU\|BJSXCxcITvd4l{KEG\|c3H5	MXyxM\|UwOTBizszN	M1j3OFQ5KGh?		MXrjZZV{\XNiY3XscEBl\WG2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?=	NHzve3g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUG5NlE5QCd-MkWxPVIyQDh:L3G+
SW480	MoDERZBweHSxc3nzJGF{e2G7	MXyxM\|UwOTBizszN	NYX3Z3dUPDhiaB?=		MXrjZZV{\XNiY3XscEBl\WG2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?=	M3n4c\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MUmyNVg5Lz5{NUG5NlE5QDxxYU6=
Colo205	Ml\pRZBweHSxc3nzJGF{e2G7	M3y3NlEwPS9zMDFOwG0>	NIrvU2k1QCCq		MoC0Z4F2e2W\|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK=	Mmf0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzOUKxPFgoRjJ3MUmyNVg5RC:jPh?=
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PCI-13	M3HDeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MoDjO\|IhcA>?	MmTjSG1UVw>?	NHjjR\|hIUTVyPUG1JOKyKDFwODFOwG0>	MofkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzM{mzPFcoRjJ3MUO5N\|g4RC:jPh?=
PCI-15B	MnvDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NVX1OVF4PzJiaB?=	MVvEUXNQ	Mn;LS2k2OD1zMTFCtUA1NjVizszN	MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTF\|OUO4O{c,OjVzM{mzPFc9N2F-
UM-SCC22B	M4XPWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MmHWO\|IhcA>?	MVTEUXNQ	MYPHTVUxRTF7INMxJFIvQSEQvF2=	MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTF\|OUO4O{c,OjVzM{mzPFc9N2F-
UM-SCC47	MnL4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MWW3NkBp	NGPnN25FVVOR	NFixW5lIUTVyPUG5JOKyKDF{LkOg{txO	MnflQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzM{mzPFcoRjJ3MUO5N\|g4RC:jPh?=
93-VU-147T	MnTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NYr6RoZsPzJiaB?=	M{LKTWROW09?	M{\qTWdKPTB;ND6zJOKyKDNwNTFOwG0>	MlLKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzM{mzPFcoRjJ3MUO5N\|g4RC:jPh?=
UD-SCC2	M3vGeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		M3vsRlczKGh?	NVmyNm42TE2VTx?=	MXvHTVUxRTJ6INMxJFIvQSEQvF2=	MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTF\|OUO4O{c,OjVzM{mzPFc9N2F-
UPCI:SCC90	NX7udZViT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MV23NkBp	NYm3XnZ5TE2VTx?=	MWjHTVUxRTZwNjFCtUAyNjVizszN	NF3Xb3M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUGzPVM5Pyd-MkWxN\|k{QDd:L3G+
RPMI-8226	NGP0cIxE\WyuIG\pZYJqdGm2eTDBd5NigQ>?	M3nuO\|EzPS9{NUCvOVAxKG6P	M2TyNVQ5cMLi	NX;MXJZxTE2VTx?=	NGrseWRl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK=	NHzZVFA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCwPFIxOid-MkWwNFgzODJ:L3G+
OPM-2	MWPD[YxtKF[rYXLpcIl1gSCDc4PhfS=>	MlnDNVI2NzJ3MD:1NFAhdk1?	NGPV[Is1QGkEoB?=	NHvySG5FVVOR	MWnk[YNz\WG\|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?	NV;aeXlkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNFgzODJpPkK1NFA5OjB{PD;hQi=>
RPMI-8226	Moe2RZBweHSxc3nzJGF{e2G7	MYGxNlUwOjVyL{WwNEBvVQ>?	NES0VVQ1QGkEoB?=	MXnEUXNQ	NHy3TphqdmS3Y3XzJINmdGxiYYDvdJRwe2m\|IHnuJIEh\G:\|ZT3k[ZBmdmSnboSgcYFvdmW{	MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTByOEKwNkc,OjVyMEiyNFI9N2F-
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COG-LL-319	NFjDd49HfW6ldHnvckBCe3OjeR?=	M1\hW\|ExOCCwTR?=	MorKNU8{NzZiaB?=	MmTuSG1UVw>?	NU\IZmp5cW6mdXPld{Bk[XOyYYPlMYRmeGWwZHXueEBO[2xvMTDjcIVifmGpZR?=	M2PV[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUWxOFczLz5{NEm1NVQ4OjxxYU6=
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RS11380	NHexfopIem:5dHigbY5pcWKrdHnvckBie3OjeR?=				M3joO2lvcGmkaYTpc44hd2ZiY3XscEBoem:5dHigbY4hcHWvYX6gVnMyOTN6MDDj[YxteyCxdnXy[ZhxemW\|c3nu[{BD[2x{IHnuJJBz\XOnbnPlJI9nKDNnIF\CV{whTUN3MDC9JFAvODF2IN88UU4>	M3:ze\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5MkW2PFM1Lz5zN{K1Olg{PDxxYU6=
FL5.12	Mkj3SpVv[3Srb36gZZN{[Xl?				NHTFTmJT\X[ncoPhcEBw\iCleYTvb4lv\SC5aYTo[JJif2GuIIDyc5Rm[3Srb36gbY4hUUx\|IHTldIVv\GWwdDDCZ4wugExib4\ldoV5eHKnc4PpcochdW:3c3WgSmw2NjF{IHPlcIx{KGmwIIDy[ZNmdmOnIH;mJIJwfmmwZTDn[YxifGmwLDDFR\|UxKD1iMD6wN{DPxE1w	NGrzTHY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{K1Olg{PCd-MUeyOVY5OzR:L3G+
FL5.12	M2rGPWZ2dmO2aX;uJIF{e2G7				NGjWOGxT\X[ncoPhcEBw\iCleYTvb4lv\SC5aYTo[JJif2GuIIDyc5Rm[3Srb36gbY4hUUx\|IHTldIVv\GWwdDDCZ4wzKG:4ZYLlfJBz\XO\|aX7nJI1wfXOnIF\MOU4yOiClZXzsd{BqdiCycnXz[Y5k\SCxZjCzKUBHSlNuIFXDOVAhRSByLkC1JO69VS5?	MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzJ3NkizOEc,OTd{NU[4N\|Q9N2F-
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NCI-H146	M{\v[GN6fG:2b4jpZ4l1gSCjc4PhfS=>		NWHKSmpEPDhiaILz		NX3SUmlPS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVkOLLVixOFYh[2WubIOgZZN{\XO\|ZXSgZZMh[2WubDD2bYFjcWyrdImgZYZ1\XJiNEigbJJ{KGmwIIDy[ZNmdmOnIH;mJFExLSCqdX3hckB{\XK3bTygSWM2OCB;IECuNFg4KM7:TT6=	MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDh2MUi4Nkc,OTh6NEG4PFI9N2F-
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Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID

Western blot	PARP / c-PARP / cleaved caspase 3 ; Hif-1a ; γ-H2AX / p-ATM	21393866 22006676 21084274
Immunofluorescence	cytochrome C ; Bax ; Bim ; AIF ; p65	26447615 25034785 28846096
Growth inhibition assay	Cell viability	22311987
ELISA	IL-6 / IL-8	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 (from 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 Research: ^[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. (Only for Reference)
Animal Research: ^[1]	Animal Models: Scid mice injected with Luc-expressing FD/ΔRaf-1:ER cells 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): 2%DMSO+40%PEG300+5%Tween80+53%ddH2O For best results, use promptly after mixing. Click to purchase: PEG300 Tween 80	2mg/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

Molecular Weight	813.43
Formula	C₄₂H₄₅ClN₆O₅S₂
CAS No.	852808-04-9
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CN(C)CCC(CSC1=CC=CC=C1)NC2=C(C=C(C=C2)S(=O)(=O)NC(=O)C3=CC=C(C=C3)N4CCN(CC4)CC5=CC=CC=C5C6=CC=C(C=C6)Cl)[N+](=O)[O-]

Download ABT-737 SDF

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Dilution Calculator Molecular Weight Calculator

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

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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.

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