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Chemistry

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Also known as: Mrtx1719, 2630904-44-6, Benzonitrile, 2-(4-(4-(aminomethyl)-1,2-dihydro-1-oxo-6-phthalazinyl)-1-methyl-1h-pyrazol-5-yl)-4-chloro-6-(cyclopropyloxy)-3-fluoro-, (2s)-, (m)-27, 2-[4-[4-(aminomethyl)-1-oxo-2h-phthalazin-6-yl]-2-methylpyrazol-3-yl]-4-chloro-6-cyclopropyloxy-3-fluorobenzonitrile, 2-(4-(4-(aminomethyl)-1-oxo-2h-phthalazin-6-yl)-2-methylpyrazol-3-yl)-4-chloro-6-cyclopropyloxy-3-fluorobenzonitrile
Molecular Formula
C23H18ClFN6O2
Molecular Weight
464.9  g/mol
InChI Key
BZKIOORWZAXIBA-UHFFFAOYSA-N
FDA UNII
UHN5PKM648

Mrtx-1719
PRMT5 Inhibitor BMS-986504 is an orally bioavailable methylthioadenosine (MTA)-selective inhibitor of the protein arginine methyltransferase 5 (PRMT5), with potential antineoplastic activity. Upon oral administration, PRMT5 inhibitor BMS-986504 targets, binds to and inhibits PRMT5 that is bound to MTA, a complex that is elevated in methylthioadenosine phosphorylase (MTAP)-deleted cancer cells, thereby specifically inhibiting the function of PRMT5 solely within MTAP-deleted cancer cells and not in normal, healthy cells. By inhibiting the methyltransferase activity of PRMT5, levels of both monomethylated and dimethylated arginine residues in histones H2A, H3 and H4 are decreased. This modulates the expression of genes involved in several cellular processes, including cellular proliferation. This may increase the expression of antiproliferative genes and/or decrease the expression of genes that promote cell proliferation, which may lead to decreased growth of rapidly proliferating cancer cells. BMS-986504 also causes dysregulated RNA splicing and decreased retinoblastoma protein (pRb). Together, this decreases proliferation and increases apoptosis specifically in MTAP-deleted cancer cells. PRMT5, a type II methyltransferase that catalyzes the formation of both omega-N monomethylarginine (MMA) and symmetric dimethylarginine (sDMA) on histones and a variety of other protein substrates involved in signal transduction and cellular transcription, is essential for the viability of cancer and normal cells. It is overexpressed in several neoplasms. Elevated levels are associated with decreased patient survival. MTAP is deleted in certain cancer cells leading to an accumulation of the metabolite MTA; MTA binds to and partially inhibits the activity of PRMT5.
1 2D Structure

Mrtx-1719

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
2-[4-[4-(aminomethyl)-1-oxo-2H-phthalazin-6-yl]-1-methylpyrazol-5-yl]-4-chloro-6-cyclopropyloxy-3-fluorobenzonitrile
2.1.2 InChI
InChI=1S/C23H18ClFN6O2/c1-31-22(20-15(8-26)19(33-12-3-4-12)7-17(24)21(20)25)16(10-28-31)11-2-5-13-14(6-11)18(9-27)29-30-23(13)32/h2,5-7,10,12H,3-4,9,27H2,1H3,(H,30,32)
2.1.3 InChI Key
BZKIOORWZAXIBA-UHFFFAOYSA-N
2.2 Other Identifiers
2.2.1 UNII
UHN5PKM648
2.3 Synonyms
2.3.1 Depositor-Supplied Synonyms

1. Mrtx1719

2. 2630904-44-6

3. Benzonitrile, 2-(4-(4-(aminomethyl)-1,2-dihydro-1-oxo-6-phthalazinyl)-1-methyl-1h-pyrazol-5-yl)-4-chloro-6-(cyclopropyloxy)-3-fluoro-, (2s)-

4. (m)-27

5. 2-[4-[4-(aminomethyl)-1-oxo-2h-phthalazin-6-yl]-2-methylpyrazol-3-yl]-4-chloro-6-cyclopropyloxy-3-fluorobenzonitrile

6. 2-(4-(4-(aminomethyl)-1-oxo-2h-phthalazin-6-yl)-2-methylpyrazol-3-yl)-4-chloro-6-cyclopropyloxy-3-fluorobenzonitrile

7. Refchem:201848

8. Mrtx 1719

9. Prmt5-mta Inhibitor Mrtx1719

10. Prmt5-mta Complex Inhibitor Mrtx1719

11. Mta-cooperative Prmt5 Inhibitor Mrtx1719

12. 2630904-45-7

13. (s)-mrtx-1719

14. Navlimetostat

15. Ay4a8wd6js

16. Unii-ay4a8wd6js

17. (2r)-2-(4-(4-(aminomethyl)-1-oxo-1,2-dihydrophthalazin-6-yl)-1-methyl-1h-pyrazol-5-yl)-4-chloro-6-cyclopropoxy-3-fluorobenzonitrile

18. 2-(4-(4-(aminomethyl)-1-oxo-1,2-dihydrophthalazin-6-yl)-1-methyl-1h-pyrazol-5-yl)-4-chloro-6-cyclopropoxy-3-fluorobenzonitrile

19. 2629314-96-9

20. Benzonitrile, 2-(4-(4-(aminomethyl)-1,2-dihydro-1-oxo-6-phthalazinyl)-1-methyl-1h-pyrazol-5-yl)-4-chloro-6-(cyclopropyloxy)-3-fluoro-, (2r)-

21. Benzonitrile, 2-[4-[4-(aminomethyl)-1,2-dihydro-1-oxo-6-phthalazinyl]-1-methyl-1h-pyrazol-5-yl]-4-chloro-6-(cyclopropyloxy)-3-fluoro-, (2r)-

22. Navlimetostat [inn]

23. Mrtx1719 Racemate

24. Mrtx1719 Hcl

25. Uhn5pkm648

26. C23h18clfn6o2

27. Mrtx-1719 Hcl

28. Orb1303284

29. Chembl5075255

30. Schembl23087302

31. Schembl29735316

32. Ex-a5505a

33. Ex-a5505b

34. Gtpl12116

35. Wlz3536

36. Glxc-25300

37. Mrtx-1719?

38. Ex-a5505

39. Mfcd34604075

40. Nsc840578

41. Nsc841295

42. Akos040757913

43. Hy-139611b

44. Nsc-840578

45. Nsc-841295

46. Ac-36984

47. Da-69270

48. Da-75760

49. Ms-28566

50. Sy310874

51. Hy-139611

52. Cs-0226219

53. Cs-0343422

54. F78345

55. (2m)-2-(4-(4-(aminomethyl)-1-oxo-1,2-dihydrophthalazin-6-yl)-1-methyl-1h-pyrazol-5-yl)-4-chloro-6-cyclopropoxy-3-fluorobenzonitrile

56. 2-[4-[4-(aminomethyl)-1-oxo-1,2-dihydrophthalazin-6-yl]-1-methyl-5-pyrazolyl]-4-chloro-6-cyclopropoxy-3-fluorobenzonitrile

57. 2-[4-[4-(aminomethyl)-1-oxo-2h-phthalazin-6-yl]-2-methyl-pyrazol-3-yl]-4-chloro-6-(cyclopropoxy)-3-fluoro-benzonitrile

58. Benzonitrile, 2-[4-[4-(aminomethyl)-1,2-dihydro-1-oxo-6-phthalazinyl]-1-methyl-1h-pyrazol-5-yl]-4-chloro-6-(cyclopropyloxy)-3-fluoro-

2.4 Create Date
2021-08-21
3 Chemical and Physical Properties
Molecular Weight 464.9 g/mol
Molecular Formula C23H18ClFN6O2
XLogP32.7
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count7
Rotatable Bond Count5
Exact Mass Da
Monoisotopic Mass Da
Topological Polar Surface Area118
Heavy Atom Count33
Formal Charge0
Complexity846
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1

ABOUT THIS PAGE

Looking for 2630904-45-7 / Mrtx-1719 API manufacturers, exporters & distributors?

Mrtx-1719 manufacturers, exporters & distributors 1

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PharmaCompass offers a list of Mrtx-1719 API manufacturers, exporters & distributors, which can be sorted by GMP, USDMF, JDMF, KDMF, CEP (COS), WC, and more, enabling you to easily find the right Mrtx-1719 manufacturer or Mrtx-1719 supplier for your needs.

Send us enquiries for free, and we will assist you in establishing a direct connection with your preferred Mrtx-1719 manufacturer or Mrtx-1719 supplier.

API | Excipient name

Mrtx-1719

Synonyms

Mrtx1719, 2630904-44-6, Benzonitrile, 2-(4-(4-(aminomethyl)-1,2-dihydro-1-oxo-6-phthalazinyl)-1-methyl-1h-pyrazol-5-yl)-4-chloro-6-(cyclopropyloxy)-3-fluoro-, (2s)-, (m)-27, 2-[4-[4-(aminomethyl)-1-oxo-2h-phthalazin-6-yl]-2-methylpyrazol-3-yl]-4-chloro-6-cyclopropyloxy-3-fluorobenzonitrile, 2-(4-(4-(aminomethyl)-1-oxo-2h-phthalazin-6-yl)-2-methylpyrazol-3-yl)-4-chloro-6-cyclopropyloxy-3-fluorobenzonitrile

Cas Number

2630904-45-7

Unique Ingredient Identifier (UNII)

UHN5PKM648

About Mrtx-1719

PRMT5 Inhibitor BMS-986504 is an orally bioavailable methylthioadenosine (MTA)-selective inhibitor of the protein arginine methyltransferase 5 (PRMT5), with potential antineoplastic activity. Upon oral administration, PRMT5 inhibitor BMS-986504 targets, binds to and inhibits PRMT5 that is bound to MTA, a complex that is elevated in methylthioadenosine phosphorylase (MTAP)-deleted cancer cells, thereby specifically inhibiting the function of PRMT5 solely within MTAP-deleted cancer cells and not in normal, healthy cells. By inhibiting the methyltransferase activity of PRMT5, levels of both monomethylated and dimethylated arginine residues in histones H2A, H3 and H4 are decreased. This modulates the expression of genes involved in several cellular processes, including cellular proliferation. This may increase the expression of antiproliferative genes and/or decrease the expression of genes that promote cell proliferation, which may lead to decreased growth of rapidly proliferating cancer cells. BMS-986504 also causes dysregulated RNA splicing and decreased retinoblastoma protein (pRb). Together, this decreases proliferation and increases apoptosis specifically in MTAP-deleted cancer cells. PRMT5, a type II methyltransferase that catalyzes the formation of both omega-N monomethylarginine (MMA) and symmetric dimethylarginine (sDMA) on histones and a variety of other protein substrates involved in signal transduction and cellular transcription, is essential for the viability of cancer and normal cells. It is overexpressed in several neoplasms. Elevated levels are associated with decreased patient survival. MTAP is deleted in certain cancer cells leading to an accumulation of the metabolite MTA; MTA binds to and partially inhibits the activity of PRMT5.

MRTX 1719 Manufacturers

A MRTX 1719 manufacturer is defined as any person or entity involved in the manufacture, preparation, processing, compounding or propagation of MRTX 1719, including repackagers and relabelers. The FDA regulates MRTX 1719 manufacturers to ensure that their products comply with relevant laws and regulations and are safe and effective to use. MRTX 1719 API Manufacturers are required to adhere to Good Manufacturing Practices (GMP) to ensure that their products are consistently manufactured to meet established quality criteria.

MRTX 1719 Suppliers

A MRTX 1719 supplier is an individual or a company that provides MRTX 1719 active pharmaceutical ingredient (API) or MRTX 1719 finished formulations upon request. The MRTX 1719 suppliers may include MRTX 1719 API manufacturers, exporters, distributors and traders.

MRTX 1719 GMP

MRTX 1719 Active pharmaceutical ingredient (API) is produced in GMP-certified manufacturing facility.

GMP stands for Good Manufacturing Practices, which is a system used in the pharmaceutical industry to make sure that goods are regularly produced and monitored in accordance with quality standards. The FDA’s current Good Manufacturing Practices requirements are referred to as cGMP or current GMP which indicates that the company follows the most recent GMP specifications. The World Health Organization (WHO) has its own set of GMP guidelines, called the WHO GMP. Different countries can also set their own guidelines for GMP like China (Chinese GMP) or the EU (EU GMP).

PharmaCompass offers a list of MRTX 1719 GMP manufacturers, exporters & distributors, which can be sorted by USDMF, JDMF, KDMF, CEP (COS), WC, and more, enabling you to easily find the right MRTX 1719 GMP manufacturer or MRTX 1719 GMP API supplier for your needs.

MRTX 1719 CoA

A MRTX 1719 CoA (Certificate of Analysis) is a formal document that attests to MRTX 1719's compliance with MRTX 1719 specifications and serves as a tool for batch-level quality control.

MRTX 1719 CoA mostly includes findings from lab analyses of a specific batch. For each MRTX 1719 CoA document that a company creates, the USFDA specifies specific requirements, such as supplier information, material identification, transportation data, evidence of conformity and signature data.

MRTX 1719 may be tested according to a variety of international standards, such as European Pharmacopoeia (MRTX 1719 EP), MRTX 1719 JP (Japanese Pharmacopeia) and the US Pharmacopoeia (MRTX 1719 USP).

Inform the supplier about your product requirements, specifying if you need a product with particular monograph like EP (Ph. Eur.), USP, JP, BP, or any other quality. In addition, clarify whether you need hydrochloride (HCl), anhydricum, base, micronisatum or a specific level of purity. To find reputable suppliers, utilize the filters and select those certified by GMP, FDA, or any other certification as per your requirement.
For your convenience, we have listed synonyms and CAS numbers to help you find the best supplier. The use of synonyms and CAS numbers can be helpful in identifying potential suppliers, but it is crucial to note that they might not always indicate the exact same product. It is important to confirm the product details with the supplier before making a purchase to ensure that it meets your requirements.
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