Momelotinib HCl

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MedKoo CAT#: 563754

CAS#: 1380317-28-1 (HCl)

Description: Momelotinib HCl is a JAK1/2 inhibitor, reducing anemia in myelofibrosis (MF) patients.

Chemical Structure

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Momelotinib HCl
CAS# 1380317-28-1 (HCl)
Instruction

Theoretical Analysis

MedKoo Cat#: 563754
Name: Momelotinib HCl
CAS#: 1380317-28-1 (HCl)
Chemical Formula: C23H24Cl2N6O2
Exact Mass: 486.13
Molecular Weight: 487.380
Elemental Analysis: C, 56.68; H, 4.96; Cl, 14.55; N, 17.24; O, 6.57

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

Related CAS #: 1056634-68-4 (free base)   1380317-28-1 (HCl)    

Synonym: Momelotinib dihydrochloride; Momelotinib HCl; CYT387 dihydrochloride; CYT387 HCl; CTY387; CYT-387; CYT 387; CYT11387; CYT-11387; CYT 11387;

IUPAC/Chemical Name: N-(Cyanomethyl)-4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]benzamide dihydrochloride

InChi Key: IPNATXQRPWRHKD-UHFFFAOYSA-N

InChi Code: InChI=1S/C23H22N6O2.2ClH/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);2*1H

SMILES Code: O=C(NCC#N)C1=CC=C(C2=NC(NC3=CC=C(N4CCOCC4)C=C3)=NC=C2)C=C1.[H]Cl.[H]Cl

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.03.00

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 487.38 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Ng K, Hendifar A, Starodub A, Chaves J, Yang Y, Koh B, Barbie D, Hahn WC, Fuchs CS. Phase 1 dose-escalation study of momelotinib, a Janus kinase 1/2 inhibitor, combined with gemcitabine and nab-paclitaxel in patients with previously untreated metastatic pancreatic ductal adenocarcinoma. Invest New Drugs. 2018 Jul 30. doi: 10.1007/s10637-018-0650-5. [Epub ahead of print] PubMed PMID: 30105668.

2: Barbie DA, Spira A, Kelly K, Humeniuk R, Kawashima J, Kong S, Koczywas M. Phase 1B Study of Momelotinib Combined With Trametinib in Metastatic, Kirsten Rat Sarcoma Viral Oncogene Homolog-Mutated Non-Small-Cell Lung Cancer After Platinum-Based Chemotherapy Treatment Failure. Clin Lung Cancer. 2018 Aug 4. pii: S1525-7304(18)30171-2. doi: 10.1016/j.cllc.2018.07.004. [Epub ahead of print] PubMed PMID: 30087028.

3: Tasian SK, Casas JA, Posocco D, Gandre-Babbe S, Gagne AL, Liang G, Loh ML, Weiss MJ, French DL, Chou ST. Mutation-specific signaling profiles and kinase inhibitor sensitivities of juvenile myelomonocytic leukemia revealed by induced pluripotent stem cells. Leukemia. 2018 Jun 8. doi: 10.1038/s41375-018-0169-y. [Epub ahead of print] PubMed PMID: 29884903.

4: Bose P, Verstovsek S. Management of Myelofibrosis-Related Cytopenias. Curr Hematol Malig Rep. 2018 Jun;13(3):164-172. doi: 10.1007/s11899-018-0447-9. Review. PubMed PMID: 29796726.

5: Chan E, Luwor R, Burns C, Kannourakis G, Findlay JK, Ahmed N. Momelotinib decreased cancer stem cell associated tumor burden and prolonged disease-free remission period in a mouse model of human ovarian cancer. Oncotarget. 2018 Mar 30;9(24):16599-16618. doi: 10.18632/oncotarget.24615. eCollection 2018 Mar 30. PubMed PMID: 29682172; PubMed Central PMCID: PMC5908273.

6: Song MK, Park BB, Uhm JE. Understanding Splenomegaly in Myelofibrosis: Association with Molecular Pathogenesis. Int J Mol Sci. 2018 Mar 18;19(3). pii: E898. doi: 10.3390/ijms19030898. Review. PubMed PMID: 29562644; PubMed Central PMCID: PMC5877759.

7: Tefferi A, Barraco D, Lasho TL, Shah S, Begna KH, Al-Kali A, Hogan WJ, Litzow MR, Hanson CA, Ketterling RP, Gangat N, Pardanani A. Momelotinib therapy for myelofibrosis: a 7-year follow-up. Blood Cancer J. 2018 Mar 7;8(3):29. doi: 10.1038/s41408-018-0067-6. PubMed PMID: 29515114; PubMed Central PMCID: PMC5841331.

8: Zheng J, Xin Y, Zhang J, Subramanian R, Murray BP, Whitney JA, Warr MR, Ling J, Moorehead L, Kwan E, Hemenway J, Smith BJ, Silverman JA. Pharmacokinetics and Disposition of Momelotinib Revealed a Disproportionate Human Metabolite-Resolution for Clinical Development. Drug Metab Dispos. 2018 Mar;46(3):237-247. doi: 10.1124/dmd.117.078899. Epub 2018 Jan 8. PubMed PMID: 29311136.

9: Spiegel JY, McNamara C, Kennedy JA, Panzarella T, Arruda A, Stockley T, Sukhai M, Thomas M, Bartoszko J, Ho J, Siddiq N, Maze D, Schimmer A, Schuh A, Sibai H, Yee K, Claudio J, Devlin R, Minden MD, Kamel-Reid S, Gupta V. Impact of genomic alterations on outcomes in myelofibrosis patients undergoing JAK1/2 inhibitor therapy. Blood Adv. 2017 Sep 8;1(20):1729-1738. doi: 10.1182/bloodadvances.2017009530. eCollection 2017 Sep 12. PubMed PMID: 29296819; PubMed Central PMCID: PMC5728340.

10: Xin Y, Kawashima J, Weng W, Kwan E, Tarnowski T, Silverman JA. Pharmacokinetics and Safety of Momelotinib in Subjects With Hepatic or Renal Impairment. J Clin Pharmacol. 2018 Apr;58(4):522-532. doi: 10.1002/jcph.1050. Epub 2017 Dec 28. PubMed PMID: 29283448.

11: Harrison CN, Vannucchi AM, Platzbecker U, Cervantes F, Gupta V, Lavie D, Passamonti F, Winton EF, Dong H, Kawashima J, Maltzman JD, Kiladjian JJ, Verstovsek S. Momelotinib versus best available therapy in patients with myelofibrosis previously treated with ruxolitinib (SIMPLIFY 2): a randomised, open-label, phase 3 trial. Lancet Haematol. 2018 Feb;5(2):e73-e81. doi: 10.1016/S2352-3026(17)30237-5. Epub 2017 Dec 20. PubMed PMID: 29275119.

12: Pardanani A, Gotlib J, Roberts AW, Wadleigh M, Sirhan S, Kawashima J, Maltzman JA, Shao L, Gupta V, Tefferi A. Long-term efficacy and safety of momelotinib, a JAK1 and JAK2 inhibitor, for the treatment of myelofibrosis. Leukemia. 2018 Apr;32(4):1035-1038. doi: 10.1038/leu.2017.330. Epub 2017 Nov 16. PubMed PMID: 29263442.

13: Steeghs EMP, Jerchel IS, de Goffau-Nobel W, Hoogkamer AQ, Boer JM, Boeree A, van de Ven C, Koudijs MJ, Besselink NJM, de Groot-Kruseman HA, Zwaan CM, Horstmann MA, Pieters R, den Boer ML. JAK2 aberrations in childhood B-cell precursor acute lymphoblastic leukemia. Oncotarget. 2017 Sep 16;8(52):89923-89938. doi: 10.18632/oncotarget.21027. eCollection 2017 Oct 27. PubMed PMID: 29163799; PubMed Central PMCID: PMC5685720.

14: Lue HW, Podolak J, Kolahi K, Cheng L, Rao S, Garg D, Xue CH, Rantala JK, Tyner JW, Thornburg KL, Martinez-Acevedo A, Liu JJ, Amling CL, Truillet C, Louie SM, Anderson KE, Evans MJ, O'Donnell VB, Nomura DK, Drake JM, Ritz A, Thomas GV. Metabolic reprogramming ensures cancer cell survival despite oncogenic signaling blockade. Genes Dev. 2017 Oct 15;31(20):2067-2084. doi: 10.1101/gad.305292.117. Epub 2017 Nov 14. PubMed PMID: 29138276; PubMed Central PMCID: PMC5733498.

15: Griesshammer M, Sadjadian P. The BCR-ABL1-negative myeloproliferative neoplasms: a review of JAK inhibitors in the therapeutic armamentarium. Expert Opin Pharmacother. 2017 Dec;18(18):1929-1938. doi: 10.1080/14656566.2017.1404574. Epub 2017 Nov 26. Review. PubMed PMID: 29134817.

16: Xin Y, Shao L, Maltzman J, Stefanidis D, Hemenway J, Tarnowski T, Deng W, Silverman JA. The Relative Bioavailability, Food Effect, and Drug Interaction With Omeprazole of Momelotinib Tablet Formulation in Healthy Subjects. Clin Pharmacol Drug Dev. 2018 Mar;7(3):277-286. doi: 10.1002/cpdd.397. Epub 2017 Oct 11. PubMed PMID: 29024542.

17: Mesa RA, Kiladjian JJ, Catalano JV, Devos T, Egyed M, Hellmann A, McLornan D, Shimoda K, Winton EF, Deng W, Dubowy RL, Maltzman JD, Cervantes F, Gotlib J. SIMPLIFY-1: A Phase III Randomized Trial of Momelotinib Versus Ruxolitinib in Janus Kinase Inhibitor-Naïve Patients With Myelofibrosis. J Clin Oncol. 2017 Dec 1;35(34):3844-3850. doi: 10.1200/JCO.2017.73.4418. Epub 2017 Sep 20. PubMed PMID: 28930494.

18: Verstovsek S, Courby S, Griesshammer M, Mesa RA, Brachmann CB, Kawashima J, Maltzman JD, Shao L, Xin Y, Huang D, Bajel A. A phase 2 study of momelotinib, a potent JAK1 and JAK2 inhibitor, in patients with polycythemia vera or essential thrombocythemia. Leuk Res. 2017 Sep;60:11-17. doi: 10.1016/j.leukres.2017.05.002. Epub 2017 May 30. PubMed PMID: 28622623.

19: Iurlo A, Cattaneo D. Treatment of Myelofibrosis: Old and New Strategies. Clin Med Insights Blood Disord. 2017 Mar 8;10:1179545X17695233. doi: 10.1177/1179545X17695233. eCollection 2017. Review. PubMed PMID: 28579852; PubMed Central PMCID: PMC5428134.

20: Saeed I, McLornan D, Harrison CN. Managing side effects of JAK inhibitors for myelofibrosis in clinical practice. Expert Rev Hematol. 2017 Jul;10(7):617-625. doi: 10.1080/17474086.2017.1337507. Epub 2017 Jun 19. Review. PubMed PMID: 28571503.