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CYT387 sulfate salt

JAK1/JAK2 inhibitor CAS# 1056636-06-6

CYT387 sulfate salt

Catalog No. BCC1506----Order now to get a substantial discount!

Product Name & Size Price Stock
CYT387 sulfate salt:10mg $208.00 In stock
CYT387 sulfate salt:20mg $354.00 In stock
CYT387 sulfate salt:50mg $832.00 In stock
CYT387 sulfate salt:100mg $1456.00 In stock
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Quality Control of CYT387 sulfate salt

Quality Control & MSDS

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Chemical structure

CYT387 sulfate salt

3D structure

Chemical Properties of CYT387 sulfate salt

Cas No. 1056636-06-6 SDF Download SDF
PubChem ID 66576992 Appearance Powder
Formula C23H26N6O10S2 M.Wt 610.62
Type of Compound N/A Storage Desiccate at -20°C
Synonyms momelotinib sulfate
Solubility DMSO : ≥ 6.2 mg/mL (10.15 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name N-(cyanomethyl)-4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]benzamide;sulfuric acid
SMILES C1COCCN1C2=CC=C(C=C2)NC3=NC=CC(=N3)C4=CC=C(C=C4)C(=O)NCC#N.OS(=O)(=O)O.OS(=O)(=O)O
Standard InChIKey XJGPMRGWDSQVTN-UHFFFAOYSA-N
Standard InChI InChI=1S/C23H22N6O2.2H2O4S/c24-10-12-25-22(30)18-3-1-17(2-4-18)21-9-11-26-23(28-21)27-19-5-7-20(8-6-19)29-13-15-31-16-14-29;2*1-5(2,3)4/h1-9,11H,12-16H2,(H,25,30)(H,26,27,28);2*(H2,1,2,3,4)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of CYT387 sulfate salt

DescriptionCYT387 sulfate salt is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, 10-fold selectivity versus JAK3 (IC50=155 nM).In Vitro:CYT387 sulfate salt inhibits growth of Ba/F3-JAK2V617F and human erythroleukemia (HEL) cells (IC50=1.5 μM) or Ba/F3-MPLW515L cells (IC50=200 nM), but has considerably less activity against BCR-ABL harboring K562 cells (IC50=58 μM) and FLT3 mutation harboring MV4-11 cells (IC50=3 μM). Proliferation of parental Ba/F3 cells (Ba/F3-wt) stimulated with IL-3 is inhibited with an IC50 value of 1.4 μM, consistent with the established role of IL-3-dependent signaling in the parental cell line[1].In Vivo:CYT387 at twice the dose used in disease model (50 and 100 mg/kg) has little to no effect on peripheral blood counts over a period of 8 weeks. Median plasma peak concentrations are 7.1 μM with the lower dose and 32.1μM with the higher dose, with a half-life of approximately 2 hours. Trough levels at 12 hours are 10nM for the 25 mg/kg and 900nM for the 50 mg/kg dose. At day 34 after transplantation, the mean white blood cell counts and hematocrit values of the entire cohort exceeded the normal range for Balb/c mice by more than 1 SD. At this point, 6 mice are sacrificed and subjected to autopsy. In the remaining animals, treatment is initiated with 25 mg/kg CYT387, 50 mg/kg CYT387, or vehicle, administered twice daily by oral gavage (12 mice per treatment group). A rapid drop of the white cell counts is apparent in both dose cohorts as early as 6 days after initiation of treatment and a decline of the hematocrit is apparent after 20 days[2]. After oral dosing, CYT387 exhibits high plasma concentrations (Cmax= 40.4 μM; Tmax=4 h), with quantitative absolute oral bioavailability and an apparent half life of 2.4 h. The high oral bioavailability, can likely be partly ascribed to the low blood clearance of CYT387 (6.3 mL/min/kg) and therefore low susceptibility to hepatic first pass metabolism[3].

References:
[1]. Pardanani A, et al. CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients. Leukemia, 2009, 23(8), 1441-1445. [2]. Tyner JW, et al. CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms. Blood, 2010, 115(25), 5232-5240. [3]. Burns CJ, et al. Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs). Bioorg Med Chem Lett. 2009 Oct 15;19(20):5887-92.

Protocol

Kinase Assay [1]
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[1].

Cell Assay [1]
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. TheTEL/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 h at 37°C with 5% CO2[1].

Animal Administration [2]
Mice[2] On day 32 after bone marrow transplantation (when all mice exhibit severe leukocytosis and erythrocytosis), mice are assigned to 3 groups such that each group has equivalent average body weight and blood counts. CYT387 is dissolved in NMP (120 mg/mL final; 1-methyl-2-pyrrolidinone, Chromasolv Plus). Subsequently, the CYT387/NMP mix is diluted with 0.14M Captisol to a concentration of 6 mg/mL and further diluted with 0.1M Captisol to a final concentration of 4 mg/mL. All 3 groups of mice (n=12 per group) are administered CYT387 by oral gavage twice daily at 10- to 12-hour intervals from day 34 after bone marrow transplantation to day 82 (end of experiment). Mice receive NMP/Captisol without CYT387 (0 mg/kg group), 25 mg/kg CYT387, or 50 mg/kg CYT387. At day 82 after bone marrow transplantation, all mice are euthanized for analysis except for 2 mice each from the 50 mg/kg and 25 mg/kg groups, which are taken off CYT387 treatment and followed for 45 additional days. For assessment of the effects of CYT387 on normal blood counts, naive Balb/c mice are administered vehicle control, 50 mg/kg, or 100 mg/kg CYT387 in an identical fashion as described for the bone marrow transplant experimental mouse cohort. Peripheral blood is drawn at day 14, 28, 42, and 56 and levels of red cells, white cells, reticulocytes, granulocytes, lymphocytes, and monocytes are analyzed.

References:
[1]. Pardanani A, et al. CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients. Leukemia, 2009, 23(8), 1441-1445. [2]. Tyner JW, et al. CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms. Blood, 2010, 115(25), 5232-5240. [3]. Burns CJ, et al. Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs). Bioorg Med Chem Lett. 2009 Oct 15;19(20):5887-92.

CYT387 sulfate salt Dilution Calculator

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CYT387 sulfate salt Molarity Calculator

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Preparing Stock Solutions of CYT387 sulfate salt

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.6377 mL 8.1884 mL 16.3768 mL 32.7536 mL 40.942 mL
5 mM 0.3275 mL 1.6377 mL 3.2754 mL 6.5507 mL 8.1884 mL
10 mM 0.1638 mL 0.8188 mL 1.6377 mL 3.2754 mL 4.0942 mL
50 mM 0.0328 mL 0.1638 mL 0.3275 mL 0.6551 mL 0.8188 mL
100 mM 0.0164 mL 0.0819 mL 0.1638 mL 0.3275 mL 0.4094 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on CYT387 sulfate salt

CYT387 is an ATP-competitive small molecule JAK1/JAK2 inhibitor with IC50 of 11 and 18 nM for JAK1 and JAK2, respectively. CYT387 is useful for treatment of myeloproliferative disorders and anti-cancer.

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Description

Momelotinib sulfate (CYT387 sulfate salt) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, 10-fold selectivity versus JAK3 (IC50=155 nM).

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