Cyt387 - CAS 1056634-68-4
Catalog number: B0084-307720
Category: Inhibitor
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Molecular Formula:
C23H22N6O2
Molecular Weight:
414.46
COA:
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Targets:
JAK
Description:
Cyt387, also called Momelotinib, under the IUPAC name N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide, is an ATP competitive inhibitor of JAK1 (IC50 = 11 nM) and JAK2 (IC50 = 18 nM) with potential antineoplastic activity, which may result in the induction of apoptosis and a reduction of tumor cell proliferation in JAK1/2-expressing tumor cells.
Appearance:
Solid powder
Synonyms:
Cyt387; Cyt 387; Cyt-387; N-(cyanomethyl)-4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]benzamide; CYT 387; CYT-387; CYT387; Momelotinib; N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide; Cyt387; 1056634-68-4; MOMELOTINIB; N-(Cyanomethyl)-4-(2-((4-morpholinophenyl)amino)pyrimidin-4-yl)benzamide; Cyt-387; CYT 387; UNII-6O01GMS00P; CHEMBL1078178; C23H22N6O2; CYT 11387; Momelotinib (CYT387); N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide; CYT 11387, Cyt-387, 1056634-68-4; N-(cyanomethyl)-4-(2-{[4-(morpholin-4-yl)phenyl]amino}pyrimidin-4-yl)benzamide; Cyt387, CYT 11387, Cyt-387; N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide; N-(Cyanomethyl)-4-(2-((4-(morpholin-4-yl)phenyl)amino)pyrimidin-4-yl)benzamide; N-(cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]benzamide; Momelotinib [USAN]; S2219_Selleck; Momelotinib (USAN/INN); MLS006011154; 6O01GMS00P; GTPL7791; SCHEMBL2237234; CTK8C0828; AOB4616; CYT387/CYT-387 QCR-259; SYN1035; HMS3244K19; HMS3244K20; HMS3244L19; CYT387, CYT11387; CYT387,CYT 11387; ABP000831; AN-507; ANW-65331; BDBM50311017; CYT-11387; RS0045; ZINC43199890; AKOS015904624; Cyt387-Supplied by Selleck Chemicals; BCP9000570; CS-0053; GS-0387; LS41099; NCGC00244257-01; 4CA-0426; AK102858; HE067505; HY-10961; KB-76370; SMR004702928; AB003377; AJ-108274; TC-154076; ST24048452; X7506; D10315; W-5616; BRD-K87737963-001-01-1; I14-17003; N-(cyanomethyl)-4-[2-(4-morpholinoanilino)pyrimidin-4-yl]benzamide; N-(cyanomethyl)-4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]benzamide; Benzamide, N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)-; 1160597-06-7
Solubility:
Soluble in DMSO
Storage:
Store at -20° C
MSDS:
Inquire
Application:
An orally bioavailable small-molecule inhibitor of Janus kinases 1 and 2 (JAK1/2) with potential antineoplastic activity (IC50s = 11 and 18 nM, respectively)
Quality Standard:
In-house standard
Quantity:
Grams-Kilos
Density:
1.292 g/cm3
InChIKey:
ZVHNDZWQTBEVRY-UHFFFAOYSA-N
InChI:
1S/C23H22N6O2/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/h1-9,11H,12-16H2,(H,25,30)(H,26,27,28)
Canonical SMILES:
O=C(NCC#N)C(C=C1)=CC=C1C2=NC(NC(C=C3)=CC=C3N4CCOCC4)=NC=C2
1.New Drugs for the Treatment of Myelofibrosis
Ruben A. Mesa. Curr Hematol Malig Rep (2010) 5:15–21
Various therapeutic strategies are being developed to try to block the proliferative stimulus associated with these MPNassociated mutations. Current testing using these inhibitors can be divided into three groups: preclinical testing (based on in vitro activity against cells containing JAK2V617F), ongoing testing in murine models, and testing in clinical trials. Between 10 and 20 agents with reported in vitro or murine-model activity are in the pipeline (Fig. 1), but we will focus on those agents in which clinical activity has already been reported in the public forum. JAK2 inhibition clinical results can be divided into two categories of agents: novel small molecules designed and tested for specificity and selectivity against JAK2 (INCB018424, XL019, TG101348, SB1518, CYT387), and agents that inhibit a variety of kinases including JAK2 (ITF2357, CEP-701).
2.The New Landscape of Therapy for Myelofibrosis
Krisstina Gowin & Robyn Emanuel & Holly Geyer & Ruben A. Mesa. Curr Hematol Malig Rep (2013) 8:325–332
CYT387 (momelotinib), a JAK2 and JAK1 inhibitor, has recently completed phase II testing and demonstrated significant efficacy in improving anemia and transfusion dependence, as well as splenomegaly and constitutional symptoms in MF patients. Dose-limiting toxicities, including elevation in lipase levels and neurological effects, continue to be investigated. Several other JAK2 inhibitors are currently undergoing clinical testing with limited data in the public domain. These include LY2784544, NS018 and BMS-911543. The results of these phase I–II studies are anticipated with great interest. Three JAK2 inhibitors have ceased further development for MF, including XL019, which was tested in 2007 and 2008 but not pursued as a result of neurologic toxicities. Similarly, testing for CEP701 and AZD1480 was halted for a variety of reasons including lack of efficacy.
3.Philadelphia-negative myeloproliferative neoplasms at the 2012 ASH meeting: a personal summary
Stefan Schmidt. memo (2013) 6:181–184
CYT387 is a JAK-1 and JAK-2 inhibitor and was investigated in a phase I/II clinical trial in MF. Updated data presented by Pardanani et al. showed that cohorts treated with 150 mg QD (N = 52), 300 mg QD (N = 60), 150 mg BID (N = 42) achieved an overall mean decrease in spleen volume of 38 % (36–46 %), which was reached after a median of 22 days of treatment and maintained for 744 days (median). A total of 68 % patients became transfusion independent of which 50 % maintained transfusion independence for at least 1 year. In addition, an increase of hemoglobin levels of at least 2 g/dL was achieved in 13 % of patients. CYT387 treated patients showed a marked improvement of constitutional symptoms after 6 months of treatment. Among the observed hematologic AEs, thrombocytopenia was most frequent constituting 22 % and 24 % of grade 1/2 and grade 3/4 AEs, respectively. Nonhematologic AEs grade 3/4 were observed in only 1 % (headache). Similarly infrequent and second most severe were diarrhea (4 %), peripheral neuropathy (2 %), and dizziness (1 %) all of which were rated grade 2. Given the efficacy in reducing spleen volume and constitutional symptoms this substance could become of particular clinical interest because of the additionally observed transfusion independence, which might significantly contribute to a further increase in quality of life (QoL).
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Chemical Structure

CAS 1056634-68-4 Cyt387

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