Mivebresib (ABBV-075)

For research use only.

Catalog No.S8400

6 publications

Mivebresib (ABBV-075) Chemical Structure

CAS No. 1445993-26-9

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.

Selleck's Mivebresib (ABBV-075) has been cited by 6 publications

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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 M1W1PWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MVG3NkBpenN? M1TsU2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTW[0MVEyKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCvZXHzeZJm\CCjZoTldkA4OiCqcoOgZpkhS2WubITpeJJmNWeubzDseY1qdmW|Y3XuZ4Uh[XO|YYmsJGlEPTB;MD6wNFE6|ryPLh?= NFXyfJM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MkKwPFYxOCd-M{KyNFg3ODB:L3G+
Kasumi-1 MVrBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M3z5TlczKGi{cx?= NF76ZoRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFvhd5VucS1zIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBk\WyuII\pZYJqdGm2eTDt[YF{fXKnZDDh[pRmeiB5MjDodpMh[nliQ3XscJRqfHKnLXfsc{BtfW2rbnXzZ4Vv[2ViYYPzZZktKEmFNUC9NE4xODZ|zszNMi=> MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OjJyOE[wNEc,OzJ{MEi2NFA9N2F-
RS4:11 MnXyRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NVmw[3N{PzJiaILz NFjNOXdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGLTOFoyOSClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHlibXXhd5Vz\WRiYX\0[ZIhPzJiaILzJIJ6KEOnbHz0bZRz\S2pbH:gcJVucW6nc3PlcoNmKGG|c3H5MEBKSzVyPUCuNFA3PM7:TT6= NV\od48{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{KyNFg3ODBpPkOyNlA5PjByPD;hQi=>
MM1S MlK5RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NIDGOXk4OiCqcoO= MWXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2PMWOgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JI1m[XO3cnXkJIFnfGW{IEeyJIhzeyCkeTDD[YxtfGm2cnWt[4xwKGy3bXnu[ZNk\W6lZTDhd5NigSxiSVO1NF0xNjByNkZOwG0v Ml7KQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzJ{MEi2NFAoRjN{MkC4OlAxRC:jPh?=
MX1 MnKyRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NGr5[|A4OiCqcoO= NGDhO25CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3YNUBk\WyuczDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSClZXzsMZRqfGW{IFfsc{Bie3OjeTygSWM2OD1yLkCxN:69VS5? NEOzfZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OU[3PFQ3OCd-Mkm2O|g1PjB:L3G+
MX1 MmDSRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MnvsO|IhcHK| MlnHRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPWEGgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KEOnbHygWIl1\XJiR3zvJIF{e2G7LDDFR|UxRTBwMEGz{txONg>? NEPWT|U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEm0PVUzOSd-Mki5OFk2OjF:L3G+
H1299 M2\nWmZ2dmO2aX;uJIF{e2G7 MmO3NlQhcHK| NHeyU2NDcW6maX7nJIFn\mmwaYT5JJRwKEKURESgbY4hcHWvYX6gTFEzQTliY3XscJMhe3SjYnz5JIV5eHKnc4PpcochTTJiYX7kJGhRXjF4LVzDVkBtfWOrZnXyZZNmKHKncH;yeIVzKGmwY4XiZZRm\CCob4KgNlQhcHK|IHL5JGJzcWeqdD3HcI8hdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7IHLhd4VlKEKURESg[Y5o[WenbXXueEBie3OjeTygTWM2OD1yLkCy{txONg>? NH6we489[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OU[3PFQ3OCd-Mkm2O|g1PjB:L3G+
H1299 NE\hfWNHfW6ldHnvckBie3OjeR?= NWTafJZ6OjRiaILz MkSxTY5pcWKrdHnvckBw\iCEUlS0JIlvKGi3bXHuJGgyOjl7IHPlcIx{KGG|c3Xzd4VlKGG|IHTlZ5Jm[XOnIHnuJGhRXiCOQ2KtSVIuTVB2MECtcYVlcWG2ZXSgeJJidnOlcnnweIlwdmGuIILldJJme3Orb36gZYZ1\XJiMkSgbJJ{KGK7IFLybYdpfC2JbH:gcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCHQ{WwQVAvODMQvF2u NEm4flc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEm0PVUzOSd-Mki5OFk2OjF:L3G+
insect cells MXPGeY5kfGmxbjDhd5NigQ>? MWXJcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IH\1cIwhdGWwZ4ToJIh2dWGwIF6teIVzdWmwYXygTIl{Pi22YXfn[YQhSlKGNDCoNkB1dyBzM{[yJJJme2mmdXXzLUBmgHC{ZYPz[YQhcW5iYnHjeYxwfmm{dYOgbY5n\WO2ZXSgbY5{\WO2IHPlcIx{KHW|aX7nJIhqe3SxbnWgTFQheGWydHnk[UBieyC|dXLzeJJifGViYomgZYxxcGFic3Py[YVvKGG|c3H5MEBKSzVyPUCuNFLPxE1w M3HxTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNUK5OVQ3Lz5|MEWyPVU1PjxxYU6=
MV411 MWLBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NXzZTXc3PzJiaILz MYnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFLSSFQue2Wwc3n0bZZmKGi3bXHuJG1XPDFzIHPlcIx{KGGodHXyJFczKGi{czDifUBES0t6IHHzd4F6NCCLQ{WwQVAvODgQvF2u MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDNzNEWxN{c,Ojh|MUS1NVM9N2F-
HL60 MknjRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MnXqO|IhcHK| NUDVcVBtSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBDWkR2LYPlcpNqfGm4ZTDoeY1idiCKTE[wJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCFQ1u4JIF{e2G7LDDJR|UxRTBwMEpOwG0v M{fHeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{G0OVE{Lz5{OEOxOFUyOzxxYU6=
HL60 M3;BRWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MWnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiONkCgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIJ6KE2WVDDhd5NigSxiSVO1NF0xNjF{zszNMi=> NHf3b2Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUi1O|g1Pid-M{G4OVc5PDZ:L3G+
SKM1 MlfPRY51cXS3bX;yJIF{e2G7 MmTwOlAhdWdxa3e= MYDBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVS12xJINmdGy|IIjlco9oemGodHXkJIlvKFOFSVSgcY92e2ViYYPz[ZN{\WRiYYOgeJVud3JiZ4Lve5RpKGmwaHnibZRqd25iYYSgOlAhdWdxa3esJJBwKGKrZDDifUBk[WyrcHXyJI1mfGixZB?= NIPaN4g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MkOyOFk6QSd-M{KzNlQ6QTl:L3G+

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
BRD4 / c-Myc / CDK6 / Bcl-xL / Bcl-2 / Mcl-1 / HEXIM1 / p21 / p27 / Cleaved PARP ; 

PubMed: 30647404     


MV4-11 cells were treated with the indicated concentrations of ABBV-075 for 24 h. Immunoblot analyses were conducted. The expression levels of β-Actin in the cell lysates served as the loading control. The numbers beneath the bands represent densitometry analysis.

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

Solubility (25°C)

In vitro DMSO 91 mg/mL (198.05 mM)
Water Insoluble
Ethanol Insoluble

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Chemical Information

Molecular Weight 459.47
Formula

C22H19F2N3O4S

CAS No. 1445993-26-9
Storage powder
in solvent
Synonyms N/A
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

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Epigenetic Reader Domain Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID