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Momelotinib (CYT387)

Name: Momelotinib (CYT387)
Brand: Selleck Chemicals
SKU: S2219
Rating: 5 (38 reviews)

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.

CAS No. 1056634-68-4

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

Purity & Quality Control

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JAK Signaling Pathway Map

Biological Activity

Description

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>?

Click to View More Cell Line Experimental Data

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.

References

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. Click to purchase: PEG300 Tween 80	2mg/ml

Chemical Information

Molecular Weight	414.46
Formula	C₂₃H₂₂N₆O₂
CAS No.	1056634-68-4
Storage	3 years	-20°C	powder
Storage	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

Download Momelotinib (CYT387) SDF

In vivo Formulation Calculator (Clear solution)

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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.

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Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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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

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