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Nirogacestat

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CHEMISTRY
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ACTIVE PHARMA INGREDIENTS

2 API Suppliers, 1 EU WC, 1 Listed Suppliers, $ API Reference Price

2 API Suppliers
1 EU WC
1 Listed Suppliers
$ API Reference Price

DEVELOPMENTS

31 Drugs in Development

31 Drugs in Development

FINISHED DOSAGE FORMULATIONS

3 FDF Dossiers, 3 FDA Orange Book

3 FDF Dossiers
3 FDA Orange Book

DIGITAL CONTENT

1 DATA COMPILATION #PharmaFlow, 29 NEWS #PharmaBuzz

media
1 DATA COMPILATION #PharmaFlow
29 NEWS #PharmaBuzz

PATENTS & EXCLUSIVITIES

78 US Patents, 6 US Exclusivities

patents
78 US Patents
6 US Exclusivities

Synopsis

ACTIVE PHARMA INGREDIENTS

API Suppliers

USDMF

CEP/COS

JDMF

EU WC

KDMF

NDC API

VMF

Listed Suppliers

API REF. PRICE (USD/KG)

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FDF

0INTERMEDIATES

FINISHED DOSAGE FORMULATIONS

FDF Dossiers

FDA Orange Book

Europe

Canada

Australia

South Africa

Listed Dossiers

DRUG PRODUCT COMPOSITIONS

REF. STANDARDS OR IMPURITIES

EDQM

USP

Others

PATENTS & EXCLUSIVITIES

US Patents

US Exclusivities

Health Canada Patents

DIGITAL CONTENT

Data Compilation #PharmaFlow

Stock Recap #PipelineProspector

Weekly News Recap #Phispers

News #PharmaBuzz

GLOBAL SALES INFORMATION

US Medicaid (USD)

Annual Reports (USD Million)

Finished Drug Prices

0RELATED EXCIPIENT COMPANIES

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Chemistry

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Also known as: Pf-03084014, 1290543-63-3, Pf-3084014, 865773-15-5, Pf 3084014, Nirogacestat [usan]

Molecular Formula

C₂₇H₄₁F₂N₅O

Molecular Weight

489.6 g/mol

InChI Key

VFCRKLWBYMDAED-REWPJTCUSA-N

FDA UNII

QZ62892OFJ

Nirogacestat is a selective gamma secretase (GS) inhibitor with potential antitumor activity. Nirogacestat binds to GS, blocking proteolytic activation of Notch receptors; Notch signaling pathway inhibition may follow, which may result in the induction of apoptosis in tumor cells that overexpress Notch. The integral membrane protein GS is a multi-subunit protease complex that cleaves single-pass transmembrane proteins, such as Notch receptors, at residues within their transmembrane domains. Overexpression of the Notch signaling pathway has been correlated with increased tumor cell growth and survival.

1 2D Structure

Nirogacestat Hydrobromide

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

(2S)-2-[[(2S)-6,8-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl]amino]-N-[1-[1-(2,2-dimethylpropylamino)-2-methylpropan-2-yl]imidazol-4-yl]pentanamide

2.1.2 InChI

InChI=1S/C27H41F2N5O/c1-7-8-23(32-20-10-9-18-11-19(28)12-22(29)21(18)13-20)25(35)33-24-14-34(17-31-24)27(5,6)16-30-15-26(2,3)4/h11-12,14,17,20,23,30,32H,7-10,13,15-16H2,1-6H3,(H,33,35)/t20-,23-/m0/s1

2.1.3 InChI Key

VFCRKLWBYMDAED-REWPJTCUSA-N

2.1.4 Canonical SMILES

CCCC(C(=O)NC1=CN(C=N1)C(C)(C)CNCC(C)(C)C)NC2CCC3=C(C2)C(=CC(=C3)F)F

2.1.5 Isomeric SMILES

CCC[C@@H](C(=O)NC1=CN(C=N1)C(C)(C)CNCC(C)(C)C)N[C@H]2CCC3=C(C2)C(=CC(=C3)F)F

2.2 Other Identifiers

2.2.1 UNII

QZ62892OFJ

2.3 Synonyms

2.3.1 MeSH Synonyms

1. 2-(5,7-difluoro-1,2,3,4-tetrahydronaphthalen-3-ylamino)-n-(1-(2-methyl-1-(neopentylamino)propan-2-yl)-1h-imidazol-4-yl)pentanamide

2. Pf 03084014

3. Pf 3084014

4. Pf-03084014

5. Pf-3084014

6. Pf03084014

7. Pf3084014

2.3.2 Depositor-Supplied Synonyms

1. Pf-03084014

2. 1290543-63-3

3. Pf-3084014

4. 865773-15-5

5. Pf 3084014

6. Nirogacestat [usan]

7. Pf 03084014

8. Pf3084014

9. Qz62892ofj

10. (s)-2-(((s)-6,8-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl)amino)-n-(1-(2-methyl-1-(neopentylamino)propan-2-yl)-1h-imidazol-4-yl)pentanamide

11. (2s)-2-[[(2s)-6,8-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl]amino]-n-[1-[1-(2,2-dimethylpropylamino)-2-methylpropan-2-yl]imidazol-4-yl]pentanamide

12. Pf-03084014 (pf-3084014)

13. (s)-2-((s)-6,8-difluoro-1,2,3,4-tetrahydronaphthalen-2-ylamino)-n-(1-(2-methyl-1-(neopentylamino)propan-2-yl)-1h-imidazol-4-yl)pentanamide

14. Unii-qz62892ofj

15. Nirogacestat (usan/inn)

16. Nirogacestat [inn]

17. Z-3181

18. Nirogacestat [who-dd]

19. Gtpl7746

20. Chembl1770916

21. Schembl13184754

22. Dtxsid60235679

23. Ex-a855

24. Pf-3084014 (y-secratase)

25. Hms3886p21

26. Bdbm50458159

27. Mfcd19980705

28. Nsc754348

29. S8018

30. Zinc38217837

31. Akos030526383

32. Ccg-269609

33. Cs-1689

34. Db12005

35. Nsc-754348

36. Ncgc00378713-01

37. 2-(5,7-difluoro-1,2,3,4-tetrahydronaphthalen-3-ylamino)-n-(1-(2-methyl-1-(neopentylamino)propan-2-yl)-1h-imidazol-4-yl)pentanamide

38. Ac-36191

39. As-56178

40. Hy-15185

41. Pf-03084014-pf-3084014

42. A11993

43. D10960

44. F17429

45. A910640

46. Nirogacestat (pf-03084014, Pf-3084014)

47. Q27088329

48. Pf-03084014;pf-3084014;865773-15-5;

49. (2s)-2-(((2s)-6,8-difluoro-1,2,3,4-tetrahydro-2-naphthalenyl)amino)-n-(1-(2-((2,2-dimethylpropyl)amino)-1,1-dimethylethyl)-1h-imidazol-4-yl)pentanamide

50. (2s)-2-{[(2s)-6,8-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl]amino}-n-(1-{1-[(2,2-dimethylpropyl)amino]-2-methylpropan-2-yl}-1h-imidazol-4-yl)pentanamide

51. Pentanamide, 2-(((2s)-6,8-difluoro-1,2,3,4-tetrahydro-2-naphthalenyl)amino)-n-(1-(2-((2,2-dimethylpropyl)amino)-1,1-dimethylethyl)-1h-imidazol-4-yl)-, (2s)-

52. Pentanamide, 2-((6,8-difluoro-1,2,3,4-tetrahydro-2-naphthalenyl)amino)-n-(1-(2-((2,2-dimethylpropyl)amino)-1,1-dimethylethyl)-1h-imidazol-4-yl)-, (2s)-

53. Pentanamide, 2-[(6,8-difluoro-1,2,3,4-tetrahydro-2-naphthalenyl)amino]-n-[1-[2-[(2,2-dimethylpropyl)amino]-1,1-dimethylethyl]-1h-imidazol-4-yl]-, (2s)

2.4 Create Date

2010-07-06

3 Chemical and Physical Properties

Molecular Formula	C₂₇H₄₁F₂N₅O
Molecular Weight	489.6 g/mol
XLogP3	4.8
Hydrogen Bond Donor Count	3
Hydrogen Bond Acceptor Count	6
Rotatable Bond Count	11
Exact Mass	489.32791727 g/mol
Monoisotopic Mass	489.32791727 g/mol
Topological Polar Surface Area	71 Å²
Heavy Atom Count	35
Formal Charge	0
Complexity	685
Isotope Atom Count	0
Defined Atom Stereocenter Count	2
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
Covalently Bonded Unit Count	1

4 Pharmacology and Biochemistry

4.1 MeSH Pharmacological Classification

Gamma Secretase Inhibitors and Modulators

Agents that suppress GAMMA-SECRETASE by inhibiting or modulating its activities. Targeted enzymatic activities include its involvement in accumulation of toxic AMYLOID BETA-PEPTIDES (e.g., Aβ42) in ALZHEIMER DISEASE and activation of NOTCH RECEPTOR mediated SIGNAL PATHWAYS in certain cancer types. (See all compounds classified as Gamma Secretase Inhibitors and Modulators.)

API SUPPLIERS

01

TAPI Technology & API Services

Israel

USDMF, CEP/COS, JDMF, EU-WC, NDC, KDMF, VMF, Others

CPhI WW Frankfurt

Booth #6.1A32

TAPI offers customized CDMO Solutions for API development and manufacturing services.

Contact Supplier

Israel

Virtual Booth

Digital Content

USDMF CEP/COS JDMF EU-WC NDC KDMF VMF Others AUDIT

Corporate PDF

02

Sai Life Sciences Limited

India

USDMF, CEP/COS, JDMF, EU-WC, NDC, KDMF, VMF, Others

Antibody Engineering

Not Confirmed

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EU WC

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Listed Suppliers

01

TAPI Technology & API Services

Israel

CPhI WW Frankfurt

Booth #6.1A32

TAPI offers customized CDMO Solutions for API development and manufacturing services.

Contact Supplier

Israel

Virtual Booth

Digital Content

Nirogacestat Hydrobromide

About the Company : Founded in 1935, TAPI Technology & API Services has a long-standing tradition of advancing health through innovation and dedication. Today, we proudly build upon this legacy, drivi...

Founded in 1935, TAPI Technology & API Services has a long-standing tradition of advancing health through innovation and dedication. Today, we proudly build upon this legacy, driving progress in the pharmaceutical industry. Leveraging our extensive experience and world-class expertise, we deliver one of the most comprehensive API portfolios in the industry. Additionally, we provide tailored CDMO services, harnessing our proficiency in diverse technologies to meet our partners' unique needs, ensuring flexibility and excellence in every project.

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Drugs in Development