Shopping Cart
- Remove All
Your shopping cart is currently empty
Momelotinib
Catalog No. T1849Cas No. 1056634-68-4
Alias LM-1149, CYT387, CYT11387
Momelotinib (LM-1149) is an orally bioavailable small-molecule inhibitor of Janus kinases 1 and 2 (JAK1/2) with IC50 of 11 nM/18 nM. JAK1/2 inhibitor CYT387 competes with JAK1/2 for ATP binding, which may result in inhibition of JAK1/2 activation, inhibition of the JAK-STAT signaling pathway, and so the induction of apoptosis and a reduction of tumor cell proliferation in JAK1/2-expressing tumor cells.
Momelotinib
Catalog No. T1849Alias LM-1149, CYT387, CYT11387Cas No. 1056634-68-4
Momelotinib (LM-1149) is an orally bioavailable small-molecule inhibitor of Janus kinases 1 and 2 (JAK1/2) with IC50 of 11 nM/18 nM. JAK1/2 inhibitor CYT387 competes with JAK1/2 for ATP binding, which may result in inhibition of JAK1/2 activation, inhibition of the JAK-STAT signaling pathway, and so the induction of apoptosis and a reduction of tumor cell proliferation in JAK1/2-expressing tumor cells.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $32 | In Stock | |
| 2 mg | $45 | In Stock | |
| 5 mg | $74 | In Stock | |
| 10 mg | $96 | In Stock | |
| 25 mg | $169 | In Stock | |
| 50 mg | $272 | In Stock | |
| 100 mg | $428 | In Stock | |
| 200 mg | $657 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $81 | In Stock |
Bulk & Custom
Add to Cart
Questions
View MoreInhibitors Related to "Momelotinib"
Tributyrin
NSC-661583, NSC661583, NSC 661583
T1967660-01-5
Tributyrin (Glyceryl tributyrate), a neutral short-chain fatty acid triglyceride, is a stable and rapidly absorbed prodrug of Butyric Acid. It diffuses through biological membranes and is metabolized by intracellular lipases, releasing effective butyrate directly into cells in vivo, exhibiting potent proapoptotic, antiproliferative, and differentiation-inducing effects.
- $50
Size
QTY
Hydroxychloroquine
Cited
2-[[4-[(7-Chloroquinolin-4-yl)amino]pentyl](ethyl)amino]ethanol
T9287118-42-3
Hydroxychloroquine (2-[[4-[(7-Chloroquinolin-4-yl)amino]pentyl](ethyl)amino]ethanol) (HCQ) is an alkalinizing lysosomatropic drug that acts by inducing apoptosis of renal cancer cells in vitro and inhibiting TLR7/9. It is a medication used to prevent and treat malaria, and it's also being studied as an experimental treatment for COVID-19.
- $30
Size
QTY
CitedGuanidine hydrochloride
Guanidinium chloride, Guanidine HCl, Aminoformamidine Hydrochloride, Aminoformamidine HCl
T041550-01-1
Guanidine hydrochloride (Aminoformamidine Hydrochloride) is a strong organic base existing primarily as guanidium ions at physiological pH. It is found in the urine as a normal product of protein metabolism. It is also used in laboratory research as a protein denaturant.
- $29
Size
QTY
Paeonol
Peonol
T2900552-41-0
Paeonol (Peonol) is an active extraction from Paeonia suffruticosa. Paeonol inhibits MAO-A and MAO-B with IC50 of 54.6 μM and 42.5 μM, respectively.
- $46
Size
QTY
Naringin Cited
Naringoside
T059510236-47-2
Naringin (Naringoside), a flavanone glycoside, exerts various of pharmacological effects such as blood lipid lowering, antioxidant activity, anticancer activity, and inhibition of cytochrome P450 enzymes.
- $35
Size
QTY
CitedStavudine
Sanilvudine, NSC 163661, d4T, BMY-27857
T14043056-17-5
Stavudine (BMY-27857), a nucleoside reverse transcriptase inhibitor analog of thymidine, has activity against HIV.
ApoptosisAutophagyHIV ProteaseNOD-like Receptor (NLR)Nucleoside Antimetabolite/AnalogReverse Transcriptase
- $33
Size
QTY
Sodium 4-phenylbutyrate Cited
TriButyrate, Sodium Phenylbutyrate, Buphenyl
T15351716-12-7
Sodium 4-phenylbutyrate (TriButyrate), a transcriptional regulator, reversibly inhibits class I and II histone deacetylases (HDACs )resulting in a global increase in gene expression, decreased cellular proliferation, increased cell differentiation, and the induction of apoptosis in susceptible tumor cell populations.
- $38
Size
QTY
CitedL-Ascorbic acid Cited
Vitamin C, L-Ascorbate, L(+)-Ascorbic acid, Ascorbic acid
T092850-81-7
L-Ascorbic acid (Vitamin C) is a natural product that is a potent reducing agent and antioxidant. L-Ascorbic acid functions in fighting bacterial infections, in detoxifying reactions, and in the formation of collagen. L-Ascorbic acid is used in the treatment of scurvy.
- $42
Size
QTY
CitedGefitinib
Cited
ZD1839
T1181184475-35-2
Gefitinib (ZD1839) is an EGFR first-generation inhibitor with oral activity that inhibits the EGFR 19 Del and L858R mutations. Gefitinib has antitumor activity and is used for the treatment of EGFR-mutated non-small-cell lung cancers. Gefitinib administration RESULTS in the development of the EGFR C797S resistance mutation.
- $50
Size
QTY
CitedTaurine
2-Aminoethanesulfonic acid
T0022107-35-7
Taurine (2-Aminoethanesulfonic acid) is an organic acid widely distributed in animal tissues and is one of the constituents of bile acids. Taurine is involved in a number of processes related to energy expenditure and muscle function, and can treat fatigue and muscles as well as improve immune function.
- $41
Size
QTY
Curcumin Cited
Turmeric yellow, Natural Yellow 3, Indian Saffron, Diferuloylmethane
T1516458-37-7
Curcumin (Natural Yellow 3) is a phenolic natural product, an inhibitor of histone acetyltransferase p300/CREB (IC50=25 μM) with specificity. Curcumin has a wide range of pharmacological activities such as antitumor, anti-inflammatory and antioxidant.
- $30
Size
QTY
Cited5-Fluorouracil Cited
NSC 19893, Fluorouracil, 5-FU, 5-Fluoracil
T098451-21-8
5-Fluorouracil (5-FU) is a uracil analog and inhibitor of DNA synthesis, exhibiting antitumor activity by affecting pyrimidine synthesis through thymidylate synthase inhibition; it induces apoptosis and autophagy.
- $30
Size
QTY
CitedSelect Batch
Purity:99.56%
Contact us for more batch information
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | Momelotinib (LM-1149) is an orally bioavailable small-molecule inhibitor of Janus kinases 1 and 2 (JAK1/2) with IC50 of 11 nM/18 nM. JAK1/2 inhibitor CYT387 competes with JAK1/2 for ATP binding, which may result in inhibition of JAK1/2 activation, inhibition of the JAK-STAT signaling pathway, and so the induction of apoptosis and a reduction of tumor cell proliferation in JAK1/2-expressing tumor cells. |
| Targets&IC50 | JAK2:18 nM, JAK1:11 nM |
| In vitro | In a murine MPN model, CYT387 normalized blood cell density, white blood cell count and spleen size and restored physiological levels of inflammatory cytokines. |
| In vivo | In vitro, CYT387 inhibited IL-3-stimulated proliferation of parental Ba/F3 cells (IC50: 1400 nM). In addition, CYT387 inhibited the growth of red lineage colonies in JAK2V617F-positive PV patients in vitro with similar effect (IC50: 2-4 μM).CYT387 inhibited IGF-1- and IL-6-induced Ras/MAPK and PI3K/AKT signaling. In primary multiple myeloma cells, CYT387 alone or in combination with the MM therapeutic agents bortezomib and melphalan induced apoptosis.CYT387 was 9-fold more selective for JAK1 and JAK2 (IC50: 11 nM and 18 nM) than the JAK3 kinase (IC50: 155 nM).CYT387 also acted on cell lines with constitutive activation of JAK2 or MPL signaling. or MPL signaling cell lines, including Ba/F3-MPLW515L cells (IC50: 200 nM), CHRF-288-11 cells (IC50: 1 nM) and Ba/F3-TEL-JAK2 cells (IC50: 700 nM), and also inhibited cell proliferation. |
| Kinase Assay | 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 | 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 |
| Alias | LM-1149, CYT387, CYT11387 |
| Molecular Weight | 414.46 |
| Formula | C23H22N6O2 |
| Cas No. | 1056634-68-4 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 69 mg/mL (166.5 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
| ||||||||||||||||||||||||||||||||||||
Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
Keywords
Preview
Related Tags: buy Momelotinib | purchase Momelotinib | Momelotinib cost | order Momelotinib | Momelotinib chemical structure | Momelotinib in vivo | Momelotinib in vitro | Momelotinib formula | Momelotinib molecular weight
- TOP
Feedback
Hello! How can I help you today? 
Copyright © 2015-2024 TargetMol Chemicals Inc. All Rights Reserved.