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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	NGWwd41E\WyuIG\pZYJqdGm2eTDBd5NigQ>?	Mn3KNlUxKG6PwrC=	MkezO\|IhcA>?	MVvEUXNQ	MVHjZZV{\WRiOUelJIxwe3Nib3[geoli[mmuaYT5JIlvKGOnbHzzJJRz[W6\|ZnXjeIVlKHerdHigRmNNPiC\|aWLORS=>	NF70clY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[1O\|I5QCd-Mk[2OVczQDh:L3G+
KG1a	NWTz[4N4S2WubDDWbYFjcWyrdImgRZN{[Xl?	MnzvNE0yOCEQvF2=	MYWyOEBp	NXXOTZg1TE2VTx?=	NFfLNoNKSzVyPUeuOlgh\|ryPLDDk[YNz\WG\|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?	NEPt[nE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW1NlcyOid-Mk[1OVI4OTJ:L3G+
Kasumi-1	NXjIe3ZnS2WubDDWbYFjcWyrdImgRZN{[Xl?	MV6wMVExKM7:TR?=	M2TyN\|I1KGh?	NXzEWXV7TE2VTx?=	MonnTWM2OD12Lki3JO69VSxiZHXjdoVie2W\|IHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz	M17LfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NUWyO\|EzLz5{NkW1NlcyOjxxYU6=
KG1a	MmTKRZBweHSxc3nzJGF{e2G7	NGf4dIgxNTFyIN88US=>	NFXYdI8zPCCq	MYPEUXNQ	NV3o[JBJcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?=	M4XNNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NUWyO\|EzLz5{NkW1NlcyOjxxYU6=
Kasumi-1	MYHBdI9xfG:\|aYOgRZN{[Xl?	NVn1[3NQOC1zMDFOwG0>	MYiyOEBp	NGX3d\|ZFVVOR	MlzEbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>?	Mn;UQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3NUK3NVIoRjJ4NUWyO\|EzRC:jPh?=
MC-3	NY\0cmpTT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MWm1M\|ExNzJyIN88US=>	NXLk[pF6OjRiaB?=	MlPvSG1UVw>?	M2r0bolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz	MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjR2N{[xOUc,OjZ2NEe2NVU9N2F-
HN22	M2TBe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Mo\QNk42NzdwNT:yNk42KM7:TR?=	NXfqRmx2OjRiaB?=	NGPCRYZFVVOR	MXXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>	M1LhVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NES3OlE2Lz5{NkS0O\|YyPTxxYU6=
MC-3	NICyNYRCeG:ydH;zbZMhSXO\|YYm=	Mm\UOU8yOC9{MDFOwG0>	MYWyOEBp	M2LHbGROW09?	MW\pcoR2[2W\|IHPhd5Bie2VvbXXkbYF1\WRiYYDvdJRwe2m\|	M1Hkb\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NES3OlE2Lz5{NkS0O\|YyPTxxYU6=
HN22	M4PKdWFxd3C2b4Ppd{BCe3OjeR?=	MnLYNk42NzdwNT:yNk42KM7:TR?=	NI\4U3czPCCq	NFPIfWNFVVOR	NYrTNVkzcW6mdXPld{Bk[XOyYYPlMY1m\GmjdHXkJIFxd3C2b4Ppdy=>	MoLkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ2NEe2NVUoRjJ4NES3OlE2RC:jPh?=
MOLT-4	M17He2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NX3CT\|VYOTBvNUCwNEBvVQ>?	M4jYRlczKGh?	MVzEUXNQ	Moi0TWM2OD1yLkG5PEDPxE1?	MkfKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ\|OUKzN\|IoRjJ4M{myN\|MzRC:jPh?=
RS4;11	MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MmHlNVAuPTByMDDuUS=>	MkHiO\|IhcA>?	MofFSG1UVw>?	MUHJR\|UxRTBwMECyJO69VQ>?	MnfLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ\|OUKzN\|IoRjJ4M{myN\|MzRC:jPh?=
JURKAT	Mnn4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NFzpOosyOC13MECwJI5O	M4HES\|czKGh?	NYnDfYFKTE2VTx?=	MUPJR\|UxRTZ4IN88US=>	MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN7MkOzNkc,OjZ\|OUKzN\|I9N2F-
CEM R	M{fFR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NES3UHoyOC13MECwJI5O	NWnhZ5F{PzJiaB?=	M1[4WWROW09?	NVTNN4lwUUN3ME21MlQh\|ryP	NF\0Sng9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO5NlM{Oid-Mk[zPVI{OzJ:L3G+
CEM S	MlTIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MorzNVAuPTByMDDuUS=>	MWK3NkBp	NXr6T3R3TE2VTx?=	MYTJR\|UxRTF{LkGg{txO	MmXpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ\|OUKzN\|IoRjJ4M{myN\|MzRC:jPh?=
MOLT-4	NVu0UGlWSXCxcITvd4l{KEG\|c3H5	M1;yclExNTFyMECgcm0>	MmqyNlQhcA>?	NWK3PWN6TE2VTx?=	NIrHOpVk[XW\|ZYOgeIhmKGOuZXH2ZYdmKG:oIFLjcE0zKGGwZDD0bIUh\G:5boLl[5Vt[XSrb36gc4YhSmOuLYjMJIFv\CCPY3ytNS=>	NHLCcWo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO5NlM{Oid-Mk[zPVI{OzJ:L3G+
CEM S	MlzrRZBweHSxc3nzJGF{e2G7	NI\Z[W8yOC1zMECwJI5O	NHLmVZQzPCCq	MXvEUXNQ	NXvOPHBK[2G3c3XzJJRp\SClbHXheoFo\SCxZjDCZ4wuOiCjbnSgeIhmKGSxd37y[Yd2dGG2aX;uJI9nKEKlbD34UEBidmRiTXPsMVE>	M{nhVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{myN\|MzLz5{NkO5NlM{OjxxYU6=
JURKAT	NHrMXnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NHHjN4oyODBvMUCwNEBvVQ>?	M1vJdlQ5KGh?	M3nQS2ROW09?	MnHjTWM2OD17NUZCtVkvOyCwTR?=	NWnFbpNtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xO\|IzPjlpPkK2NVczOjZ7PD;hQi=>
LOUCY	MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M3O0OFExOC1zMECwJI5O	MmrROFghcA>?	MV7EUXNQ	MWHJR\|UxRTN{LklCtVExNjlibl2=	M4ewZ\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUeyNlY6Lz5{NkG3NlI3QTxxYU6=
WM-115	M4e1T2NmdGxiVnnhZoltcXS7IFHzd4F6	MljDNVAxyqCwTR?=	NY\0c49rPzJiaB?=		MVzlcohidmOnczDjeZJkfW2rbj3pcoR2[2WmIHHueIkue3W{dnn2ZYzDqA>?	NWnJUoFFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xNVY4PzZpPkK2NVE3Pzd4PD;hQi=>
B16	NVjFPZR5S2WubDDWbYFjcWyrdImgRZN{[Xl?	NXLj[GRGOTBywrDuUS=>	NYXlcoY1PzJiaB?=		MVPlcohidmOnczDjeZJkfW2rbj3pcoR2[2WmIHHueIkue3W{dnn2ZYzDqA>?	MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjFzNke3Okc,OjZzMU[3O\|Y9N2F-
HL-60	MnXIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		M1fQeVczKGh?		MVfJR\|UxyqB;IEGwMlchdk1?	NIeyS3I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC0OVYxQSd-Mk[wOFU3ODl:L3G+
MOLM-13	NGD5S5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MoLuO\|IhcA>?		M3u5RmlEPTEEoE2gNlcvQSCwTR?=	M1TScVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MES1OlA6Lz5{NkC0OVYxQTxxYU6=
OCI-AML3	NGfTW5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MWG3NkBp		MYnJR\|UxyqB;IEG5OVAhdk1?	M{PNUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MES1OlA6Lz5{NkC0OVYxQTxxYU6=
BCWM.1	M3izeGFxd3C2b4Ppd{BCe3OjeR?=	MUmwMVEvPiEQvF2=	M1X4eFI1KGh?		MmjZbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>?	NX\DdGRVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4PVMzQTBpPkK1PFk{OjlyPD;hQi=>
MWCL-1	M3vRe2Fxd3C2b4Ppd{BCe3OjeR?=	NVfNXHV[OC1zLk[g{txO	NUDabJhDOjRiaB?=		NHHQOHdqdmS3Y3XzJINmdGxiYYDvdJRwe2m\|	M{PEW\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEmzNlkxLz5{NUi5N\|I6ODxxYU6=
MM.1s	M3jQO2Fxd3C2b4Ppd{BCe3OjeR?=	MnfSNE0yNjZizszN	NE[1NYczPCCq		MXHpcoR2[2W\|IHPlcIwh[XCxcITvd4l{	MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh7M{K5NEc,OjV6OUOyPVA9N2F-
HCT116	NHzXN2xHfW6ldHnvckBCe3OjeR?=	MWCzM\|ExKM7:TR?=	MYOxNuKhcMLi	MoC0SG1UVw>?	M4n6VIlv\HWlZYOgZUBld3OnLXTldIVv\GWwdDDpcoNz\WG\|ZTDpckBNSzOELVnJJINwdn[ncoPpc44h[W6mIGPRV3ROOSCmZXfyZYRifGmxbh?=	M1LLR\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{G1NFI5Lz5{NUexOVAzQDxxYU6=
HCT116 BAX BAK1 DKO	M2G2cGZ2dmO2aX;uJGF{e2G7	NWjTS4FIOy9zMDFOwG0>	NHzQSGsyOsLiaNMg	MXPEUXNQ	MV;pcoR2[2W\|IHGg[I9{\S2mZYDlcoRmdnRiaX7jdoVie2ViaX6gUGM{Si2LSTDjc453\XK\|aX;uJIFv\CCVUWPUUVEh\GWpcnHkZZRqd25?	MlPNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5MUWwNlgoRjJ3N{G1NFI5RC:jPh?=
HCT116	MlTHSpVv[3Srb36gRZN{[Xl?	NF65VIYyOCEQvF2=	MmTnNVLDqGkEoB?=	NHf6TnJFVVOR	MlvVbY5kemWjc3XzJGdHWC2OQ{PCJJB2dmO2YR?=	M4LyOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{G1NFI5Lz5{NUexOVAzQDxxYU6=
HCT116 BAX BAK1 DKO	NUPqXGd4TnWwY4Tpc44hSXO\|YYm=	MYKxNEDPxE1?	NFrTWoUyOsLiaNMg	NEi3dppFVVOR	MVPpcoNz\WG\|ZYOgS2ZRNUyFM1KgdJVv[3Sj	MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTdzNUCyPEc,OjV5MUWwNlg9N2F-
HCT116	NXf5[JNPSXW2b4DoZYd6KEG\|c3H5	MX6xNEDPxE1?	NWjYPHdrOTMEoHlCpC=>	M4HmV2ROW09?	NGfxN4NqdmS3Y3XzJIEh[2:vcHzleIUh[XW2b4DoZYdq[yC{ZYPwc45{\Q>?	MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTdzNUCyPEc,OjV5MUWwNlg9N2F-
HCT116 BAX BAK1 DKO	MYDBeZRweGijZ4mgRZN{[Xl?	M1SyW\|ExKM7:TR?=	MXOxNuKhcMLi	NIX0fW5FVVOR	M4HsTolv\HWlZYOgZUBkd22ybHX0[UBifXSxcHjh[4lkKHKnc4DvcpNm	NV\1Um9oRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3NVUxOjhpPkK1O\|E2ODJ6PD;hQi=>
U937	NHjafVhCeG:ydH;zbZMhSXO\|YYm=	NFrYVIkxNjF{NT2yJO69VQ>?	NF32T2YzPCCq		MYflcohidmOnczDETGEwYC1zMT3pcoR2[2WmIHHwc5B1d3Orcx?=	M4jybVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{G0NFI1Lz5{NUexOFAzPDxxYU6=
U937	NUXoTlBlSXCxcITvd4l{KEG\|c3H5	MknvNE42KM7:TR?=	NX\5Uo1FOjRiaB?=		NInTdpVmdmijbnPld{BkdGWjdnHn[UBw\iCSQWLQJIFv\CClYYPwZZNmNTNiYYOge4VtdCCjczDOc5hiKGyndnXs	MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTdzNECyOEc,OjV5MUSwNlQ9N2F-
HL-60 AAA-Bcl-2	NXzCfVRkSXCxcITvd4l{KEG\|c3H5	MWSwMVUh\|ryP	MoDZOFghcA>?		MlTETWM2OD1yLki3JO69de,:jHnu[JVk\XNiY3XscEBieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI>	MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTdzMUS2NEc,OjV5MUG0OlA9N2F-
HL-60 EEE-Bcl-2	NV7KSmlRSXCxcITvd4l{KEG\|c3H5	Mn\uNE02KM7:TR?=	MWm0PEBp		NFHqfYpKSzVyPUWg{txu97zOIHnu[JVk\XNiY3XscEBieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI>	MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTdzMUS2NEc,OjV5MUG0OlA9N2F-
U87	M3i2U2Z2dmO2aX;uJGF{e2G7	NWG5bo45PTBizszN	MVeyOEBp		MlTadoVlfWOnczD0bIUhdVKQQTDlfJBz\XO\|aX;uJIxmfmWuczDv[kBOVVBvMjygUW1RNTF2IHHu[EBD[2xvMh?=	NXPkcHJERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2Olc3PjNpPkK1OlY4PjZ\|PD;hQi=>
K562	NXrZcHJTS2WubDDWbYFjcWyrdImgRZN{[Xl?	M1;VNlEuOTBizszN	MV[0PEBp	MX7EUXNQ	NF;QbndKSzVyPUK2Mlch\|ryP	M13NXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NUm2OVYyLz5{NUW5OlU3OTxxYU6=
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MM.1S	MU\GeY5kfGmxbjDBd5NigQ>?	M1LqXVUxOC95NUCgcm0>	NY\VR4xOOjRxNEigbC=>	MYfEUXNQ	MoLM[I94dnKnZ4XsZZRmeyCEaX2sJJBzcW6laYDhcIx6KHSqZTDFUEBqe2:ob4Lt	M{HoflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkC4PFg5Lz5{NUKwPFg5QDxxYU6=
Clone A	MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NGq0N2cxNjMkgKO2NEDPxE1?	NFLPUnE4OiCq	NW\zXoFITE2VTx?=	NXe2SWhXUUN3ME23MlUh\|ryP	MmLiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MEi4PFIoRjJ3MkC4PFgzRC:jPh?=
CX-1	M2PJc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NHnSSXQxNjMkgKO2NEDPxE1?	MVm3NkBp	MXTEUXNQ	M4jFcGlEPTB;MT64JO69VQ>?	NGHGS3o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKwPFg5Oid-MkWyNFg5QDJ:L3G+
LS174T	MmfFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NF\pd\|AxNjMkgKO2NEDPxE1?	NGG5SYQ4OiCq	M2XmbGROW09?	M4LnTmlEPTB;MUiuN{DPxE1?	M1PLNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkC4PFgzLz5{NUKwPFg5OjxxYU6=
HT29	MW\BdI9xfG:\|aYOgRZN{[Xl?	MYGxM\|UwOTBizszN	NG\iZnk1QCCq		NET5Xmlk[XW\|ZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>	MnPLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzOUKxPFgoRjJ3MUmyNVg5RC:jPh?=
SW480	M1PpNmFxd3C2b4Ppd{BCe3OjeR?=	NWjXPG9MOS93L{GwJO69VQ>?	MXi0PEBp		MYHjZZV{\XNiY3XscEBl\WG2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?=	NF\Fd3o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUG5NlE5QCd-MkWxPVIyQDh:L3G+
Colo205	NWDmfVcySXCxcITvd4l{KEG\|c3H5	MoPaNU82NzFyIN88US=>	NFrscmo1QCCq		MnnWZ4F2e2W\|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK=	M3naeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MUmyNVg5Lz5{NUG5NlE5QDxxYU6=
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PCI-13	MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		Mk\kO\|IhcA>?	M4[2R2ROW09?	MVvHTVUxRTF3INMxJFEvQCEQvF2=	MlnPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzM{mzPFcoRjJ3MUO5N\|g4RC:jPh?=
PCI-15B	NHrme2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MlGxO\|IhcA>?	NUHkfmlQTE2VTx?=	NUjlZXBNT0l3ME2xNUDDuSB2LkWg{txO	M4j2dlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MUO5N\|g4Lz5{NUGzPVM5PzxxYU6=
UM-SCC22B	MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MV63NkBp	NEP2SXdFVVOR	NWLWTWJiT0l3ME2xPUDDuSB{Lkmg{txO	M3SxW\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MUO5N\|g4Lz5{NUGzPVM5PzxxYU6=
UM-SCC47	Mn\JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NX[xXJUzPzJiaB?=	MWXEUXNQ	Mkm5S2k2OD1zOTFCtUAyOi5\|IN88US=>	NITUfZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUGzPVM5Pyd-MkWxN\|k{QDd:L3G+
93-VU-147T	M37nV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NXLvSmV6PzJiaB?=	NWHvRppqTE2VTx?=	NETa[WhIUTVyPUSuN{DDuSB\|LkWg{txO	M2WxOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MUO5N\|g4Lz5{NUGzPVM5PzxxYU6=
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UPCI:SCC90	NFqwbGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MUe3NkBp	MWPEUXNQ	NXX5Xnh3T0l3ME22MlYhyrFiMT61JO69VQ>?	NF\4SWY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUGzPVM5Pyd-MkWxN\|k{QDd:L3G+
RPMI-8226	MYPD[YxtKF[rYXLpcIl1gSCDc4PhfS=>	MUmxNlUwOjVyL{WwNEBvVQ>?	NFvzVI41QGkEoB?=	MkfzSG1UVw>?	MlfI[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:\|ZT3k[ZBmdmSnboSgcYFvdmW{	MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTByOEKwNkc,OjVyMEiyNFI9N2F-
OPM-2	MojnR4VtdCCYaXHibYxqfHliQYPzZZk>	NXKxRZVkOTJ3L{K1NE82ODBibl2=	NITDTpM1QGkEoB?=	MlK0SG1UVw>?	NIn1emxl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK=	M4XWOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEC4NlAzLz5{NUCwPFIxOjxxYU6=
RPMI-8226	NX31XpNESXCxcITvd4l{KEG\|c3H5	NEjFZZcyOjVxMkWwM\|UxOCCwTR?=	MYm0PIjDqA>?	NX;oXXA2TE2VTx?=	NFTmNlZqdmS3Y3XzJINmdGxiYYDvdJRwe2m\|IHnuJIEh\G:\|ZT3k[ZBmdmSnboSgcYFvdmW{	MlOzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyMEiyNFIoRjJ3MEC4NlAzRC:jPh?=
OPM-2	NIL3fYRCeG:ydH;zbZMhSXO\|YYm=	Mn7yNVI2NzJ3MD:1NFAhdk1?	M2HLUFQ5cMLi	M1:wXmROW09?	NXfIcI4ycW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?=	MkjaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyMEiyNFIoRjJ3MEC4NlAzRC:jPh?=
COG-LL-319	MUnGeY5kfGmxbjDBd5NigQ>?	MUmxNFAhdk1?	MmntNU8{NzZiaB?=	Ml7GSG1UVw>?	NWDtN2QxcW6mdXPld{Bk[XOyYYPlMYRmeGWwZHXueEBO[2xvMTDjcIVifmGpZR?=	NHjUNGs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm1NVQ4Oid-MkS5OVE1PzJ:L3G+
RS4;11	MmDxSpVv[3Srb36gRZN{[Xl?	NFr3RYgyODBibl2=	MYWxM\|MwPiCq	NHvLfJNFVVOR	M{fXXolv\HWlZYOgZ4F{eGG\|ZT3k[ZBmdmSnboSgUYNtNTFiY3zlZZZi\2V?	MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl3MUS3Nkc,OjR7NUG0O\|I9N2F-
FL5.12	NXXve\|U2TnWwY4Tpc44h[XO\|YYm=				NG\FNmhT\X[ncoPhcEBw\iCleYTvb4lv\SC5aYTo[JJif2GuIIDyc5Rm[3Srb36gbY4hUUx\|IHTldIVv\GWwdDDCZ4wzKG:4ZYLlfJBz\XO\|aX7nJI1wfXOnIF\MOU4yOiClZXzsd{BqdiCycnXz[Y5k\SCxZjDic5ZqdmViZ3XsZZRqdixiRVO1NEA:KDBwMEC4JO69VS5?	MkX3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd{NU[4N\|QoRjF5MkW2PFM1RC:jPh?=
DoHH2	Mmf6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?				NEmy[pRKdmirYnn0bY9vKG:oIHPlcIwh\3Kxd4ToJIlvKGi3bXHuJGRwUEh{IHPlcIx{KG:4ZYLlfJBz\XO\|aX7nJGJkdDJiaX6gdJJme2WwY3Wgc4YhOyViRlLTMEBGSzVyIE2gNE4xODh\|IN88UU4>	MlqwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd{NU[4N\|QoRjF5MkW2PFM1RC:jPh?=
RS11380	NFTJTpVIem:5dHigbY5pcWKrdHnvckBie3OjeR?=				NFLWdIpKdmirYnn0bY9vKG:oIHPlcIwh\3Kxd4ToJIlvKGi3bXHuJHJUOTF\|OECgZ4VtdHNib4\ldoV5eHKnc4PpcochSmOuMjDpckBxemW\|ZX7j[UBw\iB\|JTDGRnMtKEWFNUCgQUAxNjBzNDFOwG0v	M{[0dlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5MkW2PFM1Lz5zN{K1Olg{PDxxYU6=
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RS11380	Ml;uS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?				MVrJcohq[mm2aX;uJI9nKGOnbHyg[5Jwf3SqIHnuJIh2dWGwIGLTNVE{QDBiY3XscJMhd3[ncnX4dJJme3OrbnegRoNtOiCrbjDwdoV{\W6lZTDv[kAyOCViSGOsJGVEPTBiPTCwMlE2KM7:TT6=	MmriQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd{NU[4N\|QoRjF5MkW2PFM1RC:jPh?=
SUDHL4	M1XOS2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7				M3\Sb2lvcGmkaYTpc44hd2ZiY3XscEBoem:5dHigbY4hcHWvYX6gV3VFUEx2IHPlcIx{KG:4ZYLlfJBz\XO\|aX7nJGJkdDJiaX6gdJJme2WwY3Wgc4YhOyViRlLTMEBGSzVyIE2gNE4zOiEQvF2u	MnXjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd{NU[4N\|QoRjF5MkW2PFM1RC:jPh?=
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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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