Momelotinib (CYT387)

Catalog No.S2219 Synonyms: LM-1149 , CYT11387

For research use only.

Momelotinib (CYT387, LM-1149 , CYT11387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3. Momelotinib (CYT387) induces apoptosis and autophagy. Phase 3.

Momelotinib (CYT387) Chemical Structure

CAS No. 1056634-68-4

Selleck's Momelotinib (CYT387) has been cited by 38 publications

Purity & Quality Control

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Biological Activity

Description Momelotinib (CYT387, LM-1149 , CYT11387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3. Momelotinib (CYT387) induces apoptosis and autophagy. Phase 3.
Targets
JAK1 [1]
(Cell-free assay)
JAK2 [1]
(Cell-free assay)
JAK3 [1]
(Cell-free assay)
11 nM 18 nM 155 nM
In vitro

CYT387 inhibits the proliferation of parental Ba/F3 cells (Ba/F3-wt) stimulated by IL-3 with IC50 of 1400 nM. Furthermore, CYT387 also causes the inhibition of cell proliferation in cell lines constitutively activated by JAK2 or MPL signaling, including Ba/F3-MPLW515L cells, CHRF-288-11 cells and Ba/F3-TEL-JAK2 cells with IC50 of 200 nM, 1 nM and 700 nM, respectively. In addition, CYT387 has been shown to inhibit erythroid colony growth in vitro from JAK2V617F-positive PV patients with similar potency with IC50 of 2μ-4 μM. [1] A recent study shows that CYT387 inhibits PI3K/AKT and Ras/MAPK signaling induced by IL-6 and IGF-1. Moreover, CYT387 induces apoptosis as a single agent and synergizes with the conventional anti-MM therapies bortezomib and melphalan in primary multiple myeloma (MM) cells. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SET2 MX;BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MVq3NkBpenN? NXyzfWl6SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTSXQzKGOnbHzzJIV5eHKnc4PpcochUkGNMjDWOlE4TiCvdYThcpQhc2mwYYPlJIFnfGW{IEeyJIhzeyCkeTDhcIFu[XJiYnz1[UBie3OjeTygTWM2OD1yLkKzNu69VS5? NYXMSWZVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm3OlIzOzhpPkG5O|YzOjN6PD;hQi=>
BAF3 NHzQUoNCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NFjzXJc4OiCqcoO= NWPDUlR5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBud3W|ZTDCRWY{KGOnbHzzJIV5eHKnc4PpcochXEWOLVrBT|Ihc2mwYYPlJIFnfGW{IEeyJIhzeyCkeTDhcIFu[XJiYnz1[UBie3OjeTygTWM2OD1yLke5PO69VS5? MneyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl5NkKyN|goRjF7N{[yNlM5RC:jPh?=
CTLL-2 NGLhcXVCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M4fxVVczKGi{cx?= NWLvTopESW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBKVC1{LYP0bY12dGG2ZXSgcY92e2ViQ2TMUE0zKGOnbHzzJIV5eHKnc4PpcochUkGNMT;KRWs{KGGodHXyJFczKGi{czDifUBidGGvYYKgZox2\SCjc4PhfUwhUUN3ME2xMlI1Qc7:TT6= MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTd4MkKzPEc,OTl5NkKyN|g9N2F-
BAF3 MmHSRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MYC3NkBpenN? MVjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IH3veZNmKEKDRkOgZ4VtdHNiZYjwdoV{e2mwZzD3bYxlKHS7cHWgTmFMOiCtaX7hd4Uh[W[2ZYKgO|IhcHK|IHL5JIFt[W2jcjDicJVmKGG|c3H5JIlvKHC{ZYPlcoNmKG:oIFnMMVMtKEmFNUC9NU41O87:TT6= NYfWZWJYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm3OlIzOzhpPkG5O|YzOjN6PD;hQi=>
HEL 92.1.7 NWXxdWRtSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NHXIXGQ4OiCqcoO= NXzjTmlFSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDISWwhQTJwMT63JINmdGy|IHX4dJJme3OrbnegTmFMOiCYNkG3SkBufXSjboSgb4lv[XOnIHHmeIVzKDd{IHjyd{BjgSCjbHHtZZIh[my3ZTDhd5NigSxiSVO1NF0yNjhyNN88UU4> MkjLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl5NkKyN|goRjF7N{[yNlM5RC:jPh?=
HEL Mk\VRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NUPoO3BLPDhiaILz MYfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiHTDDj[YxteyCjZoTldkA1QCCqcoOgZpkhS0ONLUigZZN{[XluIFnDOVA:Oi5|zszNMi=> MnrVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl7NECxNVUoRjJ7OUSwNVE2RC:jPh?=
BAF3 MYXBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NVv0flhzPzJiaILz NYTLfXRPSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBud3W|ZTDCRWY{KGOnbHzzJIV5eHKnc4PpcochXEWOLVrBT|Mhc2mwYYPlJIFnfGW{IEeyJIhzeyCkeTDhcIFu[XJiYnz1[UBie3OjeTygTWM2OD1{LkSyOe69VS5? MmXjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl5NkKyN|goRjF7N{[yNlM5RC:jPh?=
K562 MYfBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MmTvOFghcHK| MmP5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNNU[yJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCFQ1utPEBie3OjeTygTWM2OD14LkZOwG0v MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTl2MEGxOUc,Ojl7NECxNVU9N2F-
HL60 NVHX[GVoSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NXrnZm1GPDhiaILz MmPHRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKTE[wJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCFQ1utPEBie3OjeTygTWM2OD16LkROwG0v NWnp[FJ7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm5OFAyOTVpPkK5PVQxOTF3PD;hQi=>
DAOY NIjEVpZyUFSVIHHzd4F6 NYPC[405eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFTBU3kh[2WubIO= NUjSRYhQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SJ-GBM2 NInkNolyUFSVIHHzd4F6 MlXkdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO= M{DKXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
A673 MlHOdWhVWyCjc4PhfS=> MVLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>? M2HVZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC NGSzVXRyUFSVIHHzd4F6 MYrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?= M3TlNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-37 M{jucpFJXFNiYYPzZZk> NX\2RlJOeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVM4KGOnbHzz NGG3VYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-SH NYPrW5E2eUiWUzDhd5NigQ>? MYnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3TTEBk\Wyucx?= Moq5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
BT-12 M1LMeZFJXFNiYYPzZZk> MWTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSlRvMUKgZ4VtdHN? NHzTNWU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
RD NXjUPXBFeUiWUzDhd5NigQ>? NIftWlRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUlSgZ4VtdHN? MnzDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
MG 63 (6-TG R) NF3xUI9yUFSVIHHzd4F6 MoX1dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE2JIE[zJEg3NVSJIGKpJINmdGy| MoXpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh41 NX3Xd5F5eUiWUzDhd5NigQ>? Ml\rdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqNEGgZ4VtdHN? MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
BAF3 NGC0V5pHfW6ldHnvckBie3OjeR?= NUC0UoJ1UW6qaXLpeIlwdiCxZjDKRWszKFZ4MUfGJI12fGGwdDDpckBud3W|ZTDCRWY{KGOnbHzzMEBKSzVyPUGuOe69VS5? NIHpOG09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODd6MUe4M{c,S2iHTVLMQE9iRg>?
Assay
Methods Test Index PMID
Western blot p-JAK2 / JAK2 / p-STAT3 / STAT3 ; p-Src / Src 26625308
Immunofluorescence p62 / pS6 29138276
Growth inhibition assay Cell viability 20385788
In vivo In a murine MPN model, CYT387 normalizes white cell counts, hematocrit, spleen size, and restores physiologic levels of inflammatory cytokines. [3]

Protocol (from reference)

Kinase Assay:[1]
  • Cell-free kinase activity assays:

    Glutathione-S-transferase (GST)-tagged JAK kinase domains expressed in insect cells are purified before use in a peptide substrate phosphorylation assay. Assays are carried out in 384-well optiplates using an Alphascreen Protein Tyrosine Kinase P100 detection kit and a PerkinElmer Fusion Alpha instrument.

Cell Research:[1]
  • Cell lines: Ba/F3, Ba/F3-JAK2V617F and Ba/F3-MPLW515L cells
  • Concentrations: 0 to 10 μM
  • Incubation Time: 72 hours
  • Method: Ba/F3 cells expressing JAK2V617F (Ba/F3-JAK2V617F) and MPLW515L (Ba/F3-MPLW515L) mutants, as well as CHRF-288-11 (JAK2T875N) and CMK (JAK3A572V) cells are used. The TEL/JAK2 and TEL/JAK3 fusions are generated and introduced into Ba/F3 murine cells. The TEL/JAK2- or TEL/JAK3-transfected cells are cultured in Dulbecco's modified Eagle's medium (DMEM) containing 10% fetal calf serum (FCS). Ba/F3 wild-type cells are cultured in RPMI containing 10% FCS supplemented with 5 ng/mL murine IL-3. Proliferation is measured using the Alamar Blue assay after incubating for 72 hours at 37 °C with 5% CO2
Animal Research:[3]
  • Animal Models: Balb/c mice are transplanted with bone marrow transduced with a JAK2V617F retrovirus.
  • Dosages: ≤50 mg/kg
  • Administration: Administered via p.o.

Solubility (25°C)

In vitro

DMSO 74 mg/mL
(178.54 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%PEG 300+ 3% Tween80 + ddH2O
For best results, use promptly after mixing.

2mg/ml

Chemical Information

Molecular Weight 414.46
Formula

C23H22N6O2

CAS No. 1056634-68-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1COCCN1C2=CC=C(C=C2)NC3=NC=CC(=N3)C4=CC=C(C=C4)C(=O)NCC#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.)

% 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

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01236638 Completed Drug: Momelotinib Primary Myelofibrosis|Post-Polycythemia Vera Myelofibrosis|Post-Essential Thrombocythemia Myelofibrosis Sierra Oncology Inc. November 2010 Phase 2
NCT00935987 Completed Drug: CYT387 Primary Myelofibrosis|Post-Polycythemia Vera Myelofibrosis|Post-Essential Thrombocythemia Myelofibrosis Sierra Oncology Inc. November 2009 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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