CYT387 2H2SO4 salt

Product Name: CYT387 2H2SO4 salt
CAS No.: 1056636-06-6
Chemical Name: CYT387 2H2SO4 salt
Synonyms: CYT387 sulfate;CYT-387 sulfate;CYT387 H2SO4 salt;CYT387 2H2SO4 salt;Momelotinib sulfate);CYT 387 sulfate (1:2);CYT387 (sulfate salt);CYT387 sulfate salt (CYT-387 sulfate;MOMELOTINIB SULFATE (CYT387 SULFATE SALT);CYT-387 SULFATE;CYT 387 SULFATE;MOMELOTINIB SULFATE
CBNumber: CB62624121
Molecular Formula: C23H26N6O10S2
Formula Weight: 610.61674
MOL File: 1056636-06-6.mol

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CYT387 2H2SO4 salt Property

storage temp.: Store at -20°C
solubility: Soluble in DMSO
form: Powder
color: Light yellow to yellow

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0765
Product name: Momelotinibsulfate
Packaging: 5mg
Price: $96
Updated: 2021/12/16

ChemScene

Product number: CS-0765
Product name: Momelotinibsulfate
Packaging: 10mg
Price: $126
Updated: 2021/12/16

Biorbyt Ltd

Product number: orb611829
Product name: CYT387 sulfate salt
Packaging: 10mg
Price: $238
Updated: 2021/12/16

ChemScene

Product number: CS-0765
Product name: Momelotinibsulfate
Packaging: 50mg
Price: $372
Updated: 2021/12/16

Biorbyt Ltd

Product number: orb611829
Product name: CYT387 sulfate salt
Packaging: 50mg
Price: $508.3
Updated: 2021/12/16

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CYT387 2H2SO4 salt Chemical Properties,Usage,Production

Description

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).

in vitro

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

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

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 2H2SO4 salt Preparation Products And Raw materials

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1056636-06-6, CYT387 2H2SO4 saltRelated Search:

CYT387 2H2SO4 salt

CYT387 H2SO4 salt

CYT387 sulfate

CYT-387 sulfate

CYT387 (sulfate salt)

CYT 387 sulfate (1:2)

N-(Cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]benzamide sulfate (1:2)

CYT387 sulfate salt (CYT-387 sulfate

Momelotinib sulfate)

CYT-387 SULFATE;CYT 387 SULFATE;MOMELOTINIB SULFATE

MOMELOTINIB SULFATE (CYT387 SULFATE SALT)

1056636-06-6

C23H26N6O10S2

C23H22N6O22H2SO4