Mivebresib (ABBV-075)

Catalog No.S8400

For research use only.

Mivebresib (ABBV-075) is a novel BET family bromodomain inhibitor. It binds bromodomains of BRD2/4/T with similar affinities (Ki of 1-2.2 nM) and highly selective for 18 bromodomain proteins tested (Kd > 1 μM; more than 600-fold selectivity vs. BRD4), but exhibits roughly 10-fold weaker potency towards BRD3 (Ki of 12.2 nM) and has moderate activity towards CREBBP (Kd = 87 μM; 54-fold selectivity vs. BRD4). Mivebresib(ABBV-075) efficiently triggers apoptosis in various tumor cell.

Mivebresib (ABBV-075) Chemical Structure

CAS No. 1445993-26-9

Selleck's Mivebresib (ABBV-075) has been cited by 8 Publications

Purity & Quality Control

Choose Selective Epigenetic Reader Domain Inhibitors

Biological Activity

Description Mivebresib (ABBV-075) is a novel BET family bromodomain inhibitor. It binds bromodomains of BRD2/4/T with similar affinities (Ki of 1-2.2 nM) and highly selective for 18 bromodomain proteins tested (Kd > 1 μM; more than 600-fold selectivity vs. BRD4), but exhibits roughly 10-fold weaker potency towards BRD3 (Ki of 12.2 nM) and has moderate activity towards CREBBP (Kd = 87 μM; 54-fold selectivity vs. BRD4). Mivebresib(ABBV-075) efficiently triggers apoptosis in various tumor cell.
Targets
BRD2 [1] BRD4 [1] BRD-T [1]
In vitro

ABBV-075 exhibits robust single agent activity in cell viability assays across cancer cell lines derived from solid tumors, leukemia and lymphomas. It could disrupt cell cycle control leading to G1 arrest followed by senescence, inhibit oncogenesis drivers leading to apoptosis, and potentially target tumor microenvironment to provide additional therapeutic benefit[1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MV4-11 NUDnVm9bSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NFTqPVI4OiCqcoO= MVLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2YND2xNUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkhdWWjc4Xy[YQh[W[2ZYKgO|IhcHK|IHL5JGNmdGy2aYTy[U1odG9ibIXtbY5me2OnbnPlJIF{e2G7LDDJR|UxRTBwMECxPe69VS5? NWHPV|dTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{KyNFg3ODBpPkOyNlA5PjByPD;hQi=>
Kasumi-1 MlLRRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MoDCO|IhcHK| NXLHb5JGSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLZZN2dWlvMTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[2WubDD2bYFjcWyrdImgcYVie3W{ZXSgZYZ1\XJiN{KgbJJ{KGK7IFPlcIx1cXS{ZT3ncI8hdHWvaX7ld4NmdmOnIHHzd4F6NCCLQ{WwQVAvODB4M988UU4> MoHDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzJ{MEi2NFAoRjN{MkC4OlAxRC:jPh?=
RS4:11 NESz[5JCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M4rJUFczKGi{cx?= MnzERY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCUU{S6NVEh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KG2nYYP1doVlKGGodHXyJFczKGi{czDifUBE\WyudHn0doUu\2yxIHz1cYlv\XOlZX7j[UBie3OjeTygTWM2OD1yLkCwOlTPxE1w MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OjJyOE[wNEc,OzJ{MEi2NFA9N2F-
MM1S M4jubmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MVi3NkBpenN? NFPLVmZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3NNXMh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KG2nYYP1doVlKGGodHXyJFczKGi{czDifUBE\WyudHn0doUu\2yxIHz1cYlv\XOlZX7j[UBie3OjeTygTWM2OD1yLkCwOlXPxE1w MoHSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzJ{MEi2NFAoRjN{MkC4OlAxRC:jPh?=
MX1 NUDh[opSSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NW\uSnlmPzJiaILz NGPYXGtCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3YNUBk\WyuczDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSClZXzsMZRqfGW{IFfsc{Bie3OjeTygSWM2OD1yLkCxN:69VS5? NWHFblF1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm2O|g1PjBpPkK5Olc5PDZyPD;hQi=>
MX1 MYXBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MYS3NkBpenN? MVfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2[MTDj[YxteyCjZoTldkA4OiCqcoOgZpkhS2WubDDUbZRmeiCJbH:gZZN{[XluIFXDOVA:OC5yMUROwG0v MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDl2OUWyNUc,Ojh7NEm1NlE9N2F-
H1299 MonuSpVv[3Srb36gZZN{[Xl? MYGyOEBpenN? NXHFcFB1SmmwZHnu[{Bi\m[rbnn0fUB1dyCEUlS0JIlvKGi3bXHuJGgyOjl7IHPlcIx{KHO2YXLsfUBmgHC{ZYPzbY5oKEV{IHHu[EBJWFZzNj3MR3IhdHWlaX\ldoF{\SC{ZYDvdpRmeiCrbnP1ZoF1\WRiZn;yJFI1KGi{czDifUBDemmpaIStS4xwKGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTDiZZNm\CCEUlS0JIVv\2GpZX3lcpQh[XO|YYmsJGlEPTB;MD6wNu69VS5? NYLBWJhRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm2O|g1PjBpPkK5Olc5PDZyPD;hQi=>
H1299 MnnkSpVv[3Srb36gZZN{[Xl? MoXxNlQhcHK| NFe3bmRKdmirYnn0bY9vKG:oIFLSSFQhcW5iaIXtZY4hUDF{OUmgZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4hUFCYIFzDVk1GOi2HUESwNE1u\WSrYYTl[EB1emGwc3PybZB1cW:wYXygdoVxemW|c3nvckBi\nSncjCyOEBpenNiYomgRpJq\2i2LVfsc{BtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFXDOVA:OC5yMt88UU4> Mn;EQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh7NEm1NlEoRjJ6OUS5OVIyRC:jPh?=
insect cells NFrqN21HfW6ldHnvckBie3OjeR?= M{nh[mlvcGmkaYTpc44hd2ZicnXjc41jcW6jboSg[pVtdCCuZX7neIghcHWvYX6gUk11\XKvaX7hcEBJcXN4LYTh[4dm\CCEUlS0JEgzKHSxIEGzOlIhemW|aXT1[ZMqKGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{Bqdm[nY4Tl[EBqdnOnY4SgZ4VtdHNidYPpcochcGm|dH;u[UBJPCCyZYD0bYRmKGG|IIP1ZpN1emG2ZTDifUBidHCqYTDzZ5Jm\W5iYYPzZZktKEmFNUC9NE4xOs7:TT6= MmHiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB3Mkm1OFYoRjNyNUK5OVQ3RC:jPh?=
MV411 Mnj2RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NVL3S5k6PzJiaILz NH\OVHdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JGJTTDRvc3Xud4l1cX[nIHj1cYFvKE2YNEGxJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCFQ1u4JIF{e2G7LDDJR|UxRTBwMEhOwG0v M37XPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{G0OVE{Lz5{OEOxOFUyOzxxYU6=
HL60 MkjnRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M3jVflczKGi{cx?= M4H3RmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgRnJFPC2|ZX7zbZRqfmViaIXtZY4hUEx4MDDj[YxteyCjZoTldkA4OiCqcoOgZpkhS0ONODDhd5NigSxiSVO1NF0xNjB7zszNMi=> NXLBcHVORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizNVQ2OTNpPkK4N|E1PTF|PD;hQi=>
HL60 NX[5SlY1SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= Mli2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKTE[wJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBjgSCPVGSgZZN{[XluIFnDOVA:OC5zMt88UU4> MmXRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF6NUe4OFYoRjNzOEW3PFQ3RC:jPh?=
SKM1 NUHhbnJOSW62aYT1cY9zKGG|c3H5 M{LYSVYxKG2pL3vn M3eybWFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLUVEh[2WubIOgfIVvd2e{YX\0[YQhcW5iU1PJSEBud3W|ZTDhd5Nme3OnZDDhd{B1fW2xcjDndo94fGhiaX7obYJqfGmxbjDheEA3OCCvZz;r[{wheG9iYnnkJIJ6KGOjbHnw[ZIhdWW2aH;k NYHPfnlGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{KzNlQ6QTlpPkOyN|I1QTl7PD;hQi=>
Assay
Methods Test Index PMID
Western blot BRD4 / c-Myc / CDK6 / Bcl-xL / Bcl-2 / Mcl-1 / HEXIM1 / p21 / p27 / Cleaved PARP 30647404
In vivo ABBV-075 has comparable or superior efficacies to standard of care agents in flank xenograft mouse models of non-small-cell and small cell lung cancers, pancreatic, breast, prostate, head & neck cancers, multiple myeloma, diffuse large B cell lymphoma and leukemia[1].

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 459.47
Formula

C22H19F2N3O4S

CAS No. 1445993-26-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCS(=O)(=O)NC1=CC(=C(C=C1)OC2=C(C=C(C=C2)F)F)C3=CN(C(=O)C4=C3C=CN4)C

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04480086 Active not recruiting Drug: Mivebresib|Drug: Navitoclax|Drug: Ruxolitinib Myelofibrosis (MF) AbbVie March 17 2021 Phase 1
NCT02391480 Completed Drug: ABBV-075|Drug: Venetoclax Cancer|Breast Cancer|Non-Small Cell Lung Cancer|Acute Myeloid Leukemia (AML)|Multiple Myeloma|Prostate Cancer|Small Cell Lung Cancer|Non-Hodgkins Lymphoma AbbVie April 14 2015 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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