Momelotinib

SKU: orb1307329

Description

Momelotinib (CYT387) is a potent and orally bioavailable JAK1/2 inhibitor (IC50: 11 nM/18 nM) that blocks ATP binding, disrupting JAK-STAT signaling. This action leads to inhibited proliferation and induced apoptosis in relevant tumor cells, as demonstrated in cellular and animal models of myeloproliferative neoplasms.

Research Area

Cardiovascular Research, Cell Biology, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Images & Validation

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Key Properties

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CAS Number	1056634-68-4
MW	414.46
Purity	98.75%
Formula	C₂₃H₂₂N₆O₂
SMILES	O=C(NCC#N)c1ccc(cc1)-c1ccnc(Nc2ccc(cc2)N2CCOCC2)n1
Target	Autophagy,JAK,Apoptosis
Solubility	DMSO:62.5 mg/mL (150.8 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.41 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

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Target IC50	JAK3:155 nM\|JAK1:11 nM\|JAK2:18 nM
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. Read more...
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. Read more...
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 Read more...

Storage & Handling

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Storage	store at low temperature \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Momelotinib, JAK3, Janus kinase, JAK1, JAK2, JAK, inhibit, LM 1149, LM1149, LM-1149, Inhibitor, Apoptosis, Autophagy, CYT 11387, CYT 387, CYT387, CYT-387, CYT11387, CYT-11387

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Compound Identifiers

PubChem CID

25062766 ↗

Key Properties

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No computed properties available.

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CAS Number:	1056636-06-6
MW:	610.62
Formula:	C₂₃H₂₆N₆O₁₀S₂

CAS Number:	1056636-07-7
MW:	510.57
Formula:	C₂₄H₂₆N₆O₅S

CAS Number:	1380317-28-1
MW:	487.38
Formula:	C₂₃H₂₄Cl₂N₆O₂

Momelotinib

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

Similar Products

Momelotinib sulfate [orb1707408]

Momelotinib Mesylate [orb1707409]

Momelotinib HCl [orb1738657]

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