Evobrutinib (M-2951)

Catalog No.S8777 Synonyms: MSC-2364447C

For research use only.

Evobrutinib (M-2951, MSC-2364447C) is a highly selective BTK inhibitor with an IC50 of 37.9 nM. It has potential anti-neoplastic activity.

Evobrutinib (M-2951) Chemical Structure

CAS No. 1415823-73-2

Selleck's Evobrutinib (M-2951) has been cited by 1 Publication

Purity & Quality Control

Choose Selective BTK Inhibitors

Biological Activity

Description Evobrutinib (M-2951, MSC-2364447C) is a highly selective BTK inhibitor with an IC50 of 37.9 nM. It has potential anti-neoplastic activity.
Targets
BTK [1]
(Cell-free assay)
37.9 nM
In vitro

Evobrutinib can inhibit the activity of BTK and prevent the activation of the BCR signaling pathway. It is metabolized via hydroxylation, hydrolysis, O-dealkylation, glucuronidation, and GSH conjugation[2].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
THP1 M3HNOGZ2dmO2aX;uJIF{e2G7 MlTNNlQhcHK| NFjKW2NKdmirYnn0bY9vKG:oIFLUT{BqdiC4aYThcYlvKER|IHTp[oZmemWwdHnheIVlKGi3bXHuJHRJWDFiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBHS2ejbX3hVk1qdmS3Y3XkJGlNQCCycn;keYN1cW:wIH3lZZN2emWmIHHmeIVzKDJ2IHjyd{BjgSCKVGLGJIF{e2G7LDDJR|UxRTBwME[x{txO NF\WS3c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MkC4N|g2QCd-M{KwPFM5PTh:L3G+
PBMC M4jSVGZ2dmO2aX;uJIF{e2G7 MojQOlAhdWmwcx?= MVnJcohq[mm2aX;uJI9nKEKWSzDpckBpfW2jbjDQRm1EKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDhcpRqNUmpTT3zeIlufWyjdHXkJGNFPjliZYjwdoV{e2mxbjDvckBDKGOnbHzzJJBz\WmwY4XiZZRm\CCob4KgOlAhdWmwczDmc4xtd3enZDDifUBod2G2IF[oZYIoMTJiYX70bU1pfW2jbjDJ[20he3SrbYXsZZRqd25iYX7kJI1m[XO3cnXkJIFnfGW{IH;2[ZJvcWeqdDDpcoN2[mG2aX;uJIJ6KG[ub4egZ5l1d22ndIL5MEBKSzVyPUCuNFYy|ryP MoDNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF|Nki3NFUoRjNzM{[4O|A2RC:jPh?=
B cells M2XIPGZ2dmO2aX;uJIF{e2G7 M4PWeFYxKG2rboO= Mki2TY5pcWKrdHnvckBw\iCEVFugbY4hcHWvYX6gRkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iYX70bU1K\01xSVy0MZN1cW23bHH0[YQhS0R4OTDlfJBz\XO|aX;uJI9vKEJiY3XscJMheHKnaX7jeYJifGWmIH\vdkA3OCCvaX7zJIZwdGyxd3XkJIJ6KGGwdHmtTYdOKGGwdHnic4R6N0mONDDzeIlufWyjdHnvckBidmRibXXhd5Vz\WRiYX\0[ZIhOTZiaILzJIJ6KG[ub4egZ5l1d22ndIL5MEBKSzVyPUCuN|LPxE1? NEfLOHA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MkC4N|g2QCd-M{KwPFM5PTh:L3G+
HEK293 M4XxUGZ2dmO2aX;uJIF{e2G7 MnnCTY5pcWKrdHnvckBw\iCqdX3hckBGWkdiZYjwdoV{e2WmIHnuJGhGUzJ7MzDj[YxteyCjdDCtPFAhdVZiaH;s[Ilv\yCyb4TlcpRq[WxiYomgTHBNSyCjbnHsfZNqeyxiS3m9N{4y|ryP NVHqVplORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{GzOlg4ODVpPkOxN|Y5PzB3PD;hQi=>
Sf21 NYrScIp5TnWwY4Tpc44h[XO|YYm= M1rVd2lvcGmkaYTpc44hd2ZiTj30[ZJucW6jbDDHV3QufGGpZ3XkJIh2dWGwIFXHSnIhMDZ7NjD0c{BmdmRiYX3pco9i[2mmczmg[ZhxemW|c3XkJIlvKGKjY4Xsc5ZqenW|IHnu[oVkfGWmIGPmNlEh[2WubIOsJGlEPTB;NT64{txO NHzYWWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUO2PFcxPSd-M{GzOlg4ODV:L3G+
BTI-TN-5B1-4 MUTGeY5kfGmxbjDhd5NigQ>? NHvHT|hEd3[jbHXueEBjcW6maX7nJIFn\mmwaYT5JJRwKGi3bXHuJGJVUyBqM{iyJJRwKDZ3OTDy[ZNq\HWnczmg[ZhxemW|c3XkJIlvKGKjY4Xsc5ZqenW|IHnu[oVkfGWmIFLUTU1VVi13QkGtOEBqdnOnY4SgZ4VtdHNiYomgbZNwfGincn3hcEBk[Wyxcnnt[ZRzgQ>? M1q3WVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzM{[4O|A2Lz5|MUO2PFcxPTxxYU6=
Sf21 M1joNGZ2dmO2aX;uJIF{e2G7 MVWxJJVO MWnJcohq[mm2aX;uJI9nKE5vdHXycYlv[WxiSHnzOk11[WepZXSg[pVtdCCuZX7neIghcHWvYX6gRm1ZKGW6cILld5Nm\CCrbjDT[lIyKGOnbHzzJIF1KDFidV2= MlzTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF|Nki3NFUoRjNzM{[4O|A2RC:jPh?=
Sf21 MlG1SpVv[3Srb36gZZN{[Xl? MWmxJJVO MXPJcohq[mm2aX;uJI9nKE5vdHXycYlv[WxiSHnzOk11[WepZXSgbJVu[W5iVFXDJEgyPzRidH:g[Y5lKGGvaX7vZYNq\HNrIHX4dJJme3OnZDDpckBj[WO3bH;2bZJ2eyCrbn\lZ5Rm\CCVZkKxJINmdGy|IHH0JFEhfU1? MoryQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF|Nki3NFUoRjNzM{[4O|A2RC:jPh?=

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 429.51
Formula

C25H27N5O2

CAS No. 1415823-73-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C=CC(=O)N1CCC(CC1)CNC2=NC=NC(=C2C3=CC=C(C=C3)OC4=CC=CC=C4)N

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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.)

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%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
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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05248945 Recruiting Drug: Evobrutinib|Drug: Carbamazepine Healthy Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany January 13 2022 Phase 1
NCT04546789 Completed Drug: M2951 (BTK inhibitor) Hepatic Impairment Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany September 30 2020 Phase 1
NCT04314024 Completed Drug: Evobrutinib Healthy Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany May 25 2020 Phase 1
NCT03934502 Completed Drug: Evobrutinib Healthy Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany April 15 2019 Phase 1

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

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

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