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Chemistry

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Also known as: Kpt-9274, 1643913-93-2, Padnarsertib, Kpt9274, Kpt 9274, (e)-3-(6-aminopyridin-3-yl)-n-((5-(4-(4,4-difluoropiperidine-1-carbonyl)phenyl)-7-(4-fluorophenyl)benzofuran-2-yl)methyl)acrylamide
Molecular Formula
C35H29F3N4O3
Molecular Weight
610.6  g/mol
InChI Key
MRFOPLWJZULAQD-SWGQDTFXSA-N
FDA UNII
9T56TV18X7

KPT-9274
Padnarsertib is an orally bioavailable inhibitor of both the serine/threonine kinase P21-activated kinase 4 (PAK4) and the nicotinamide adenine dinucleotide (NAD)-synthesizing enzyme nicotinamide phosphoribosyltransferase (NAMPT; NAMPRTase), with potential antineoplastic activity. Upon administration, padnarsertib allosterically binds to, destabilizes and causes degradation of PAK4. This inhibits PAK4-mediated signaling, induces cell death in, and inhibits the proliferation of PAK4-overexpressing tumor cells. In addition, padnarsertib binds to and inhibits the activity of NAMPT. This depletes cellular NAD and inhibits NAD-dependent enzymes, both of which are needed for rapid cell proliferation; this results in tumor cell death in NAMPT-overexpressing cancer cells. PAK4, a serine/threonine kinase and member of the PAK family of proteins upregulated in various cancer cell types, regulates cell motility, proliferation and survival. NAMPT, an enzyme that is responsible for maintaining the intracellular NAD pool, plays a key role in the regulation of cellular metabolism and has cytokine-like activities. NAMPT is often overexpressed in a variety of cancers and metabolic disorders and tumor cells rely on NAMPT activity for their NAD supply.
1 2D Structure

KPT-9274

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
(E)-3-(6-aminopyridin-3-yl)-N-[[5-[4-(4,4-difluoropiperidine-1-carbonyl)phenyl]-7-(4-fluorophenyl)-1-benzofuran-2-yl]methyl]prop-2-enamide
2.1.2 InChI
InChI=1S/C35H29F3N4O3/c36-28-9-7-24(8-10-28)30-19-26(23-3-5-25(6-4-23)34(44)42-15-13-35(37,38)14-16-42)17-27-18-29(45-33(27)30)21-41-32(43)12-2-22-1-11-31(39)40-20-22/h1-12,17-20H,13-16,21H2,(H2,39,40)(H,41,43)/b12-2+
2.1.3 InChI Key
MRFOPLWJZULAQD-SWGQDTFXSA-N
2.1.4 Canonical SMILES
C1CN(CCC1(F)F)C(=O)C2=CC=C(C=C2)C3=CC(=C4C(=C3)C=C(O4)CNC(=O)C=CC5=CN=C(C=C5)N)C6=CC=C(C=C6)F
2.1.5 Isomeric SMILES
C1CN(CCC1(F)F)C(=O)C2=CC=C(C=C2)C3=CC(=C4C(=C3)C=C(O4)CNC(=O)/C=C/C5=CN=C(C=C5)N)C6=CC=C(C=C6)F
2.2 Other Identifiers
2.2.1 UNII
9T56TV18X7
2.3 Synonyms
2.3.1 MeSH Synonyms

1. Kpt-9274

2.3.2 Depositor-Supplied Synonyms

1. Kpt-9274

2. 1643913-93-2

3. Padnarsertib

4. Kpt9274

5. Kpt 9274

6. (e)-3-(6-aminopyridin-3-yl)-n-((5-(4-(4,4-difluoropiperidine-1-carbonyl)phenyl)-7-(4-fluorophenyl)benzofuran-2-yl)methyl)acrylamide

7. 9t56tv18x7

8. (e)-3-(6-aminopyridin-3-yl)-n-[[5-[4-(4,4-difluoropiperidine-1-carbonyl)phenyl]-7-(4-fluorophenyl)-1-benzofuran-2-yl]methyl]prop-2-enamide

9. 2-propenamide, 3-(6-amino-3-pyridinyl)-n-((5-(4-((4,4-difluoro-1-piperidinyl)carbonyl)phenyl)-7-(4-fluorophenyl)-2-benzofuranyl)methyl)-, (2e)-

10. 2-propenamide, 3-(6-amino-3-pyridinyl)-n-[[5-[4-[(4,4-difluoro-1-piperidinyl)carbonyl]phenyl]-7-(4-fluorophenyl)-2-benzofuranyl]methyl]-, (2e)-

11. 2226508-53-6

12. 3-(6-aminopyridin-3-yl)-n-((5-(4-(4,4-difluoropiperidine-1-carbonyl)phenyl)-7-(4-fluorophenyl)benzofuran-2-yl)methyl)acrylamide

13. (~{e})-3-(6-azanylpyridin-3-yl)-~{n}-[[5-[4-[4,4-bis(fluoranyl)piperidin-1-yl]carbonylphenyl]-7-(4-fluorophenyl)-1-benzofuran-2-yl]methyl]prop-2-enamide

14. Padnarsertib [inn]

15. Unii-9t56tv18x7

16. Chembl4297467

17. Pak4-in-1kpt9274

18. Schembl16345416

19. Schembl16348032

20. Gtpl10593

21. Ex-a563

22. Kpt 9274 [who-dd]

23. Bcp10637

24. Kpt 9274;kpt9274

25. Mfcd30207881

26. Nsc792970

27. S8444

28. Zinc253387914

29. Ccg-270228

30. Cs-5146

31. Nsc-792970

32. Ncgc00484085-01

33. Ncgc00484085-02

34. Ac-35883

35. As-79230

36. Hy-12793

37. A857869

38. J-690230

39. (2e)-3-(6-amino-3-pyridinyl)-n-((5-(4-((4,4-difluoro-1-piperidinyl)carbonyl)phenyl)-7-(4-fluorophenyl)-2-benzofuranyl)methyl)-2-propenamide

40. 3-(6-amino-3-pyridinyl)-n-[[5-[4-[(4,4-difluoro-1-piperidinyl)carbonyl]phenyl]-7-(4-fluorophenyl)-2-benzofuranyl]methyl]-, (2e)-2-propenamide​

41. 4-(4-chlorophenyl)-2,3,9-trimethyl-6h-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide

2.4 Create Date
2016-02-23
3 Chemical and Physical Properties
Molecular Weight 610.6 g/mol
Molecular Formula C35H29F3N4O3
XLogP36.1
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count8
Rotatable Bond Count7
Exact Mass610.21917529 g/mol
Monoisotopic Mass610.21917529 g/mol
Topological Polar Surface Area102 Ų
Heavy Atom Count45
Formal Charge0
Complexity1040
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count1
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1

ABOUT THIS PAGE

Looking for 1643913-93-2 / KPT-9274 API manufacturers, exporters & distributors?

KPT-9274 manufacturers, exporters & distributors 1

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PharmaCompass offers a list of KPT-9274 API manufacturers, exporters & distributors, which can be sorted by GMP, USDMF, JDMF, KDMF, CEP (COS), WC, Price,and more, enabling you to easily find the right KPT-9274 manufacturer or KPT-9274 supplier for your needs.

Send us enquiries for free, and we will assist you in establishing a direct connection with your preferred KPT-9274 manufacturer or KPT-9274 supplier.

PharmaCompass also assists you with knowing the KPT-9274 API Price utilized in the formulation of products. KPT-9274 API Price is not always fixed or binding as the KPT-9274 Price is obtained through a variety of data sources. The KPT-9274 Price can also vary due to multiple factors, including market conditions, regulatory modifications, or negotiated pricing deals.

API | Excipient name

KPT-9274

Synonyms

1643913-93-2, Padnarsertib, Kpt9274, Kpt 9274, (e)-3-(6-aminopyridin-3-yl)-n-((5-(4-(4,4-difluoropiperidine-1-carbonyl)phenyl)-7-(4-fluorophenyl)benzofuran-2-yl)methyl)acrylamide, 9t56tv18x7

Cas Number

1643913-93-2

Unique Ingredient Identifier (UNII)

9T56TV18X7

About KPT-9274

Padnarsertib is an orally bioavailable inhibitor of both the serine/threonine kinase P21-activated kinase 4 (PAK4) and the nicotinamide adenine dinucleotide (NAD)-synthesizing enzyme nicotinamide phosphoribosyltransferase (NAMPT; NAMPRTase), with potential antineoplastic activity. Upon administration, padnarsertib allosterically binds to, destabilizes and causes degradation of PAK4. This inhibits PAK4-mediated signaling, induces cell death in, and inhibits the proliferation of PAK4-overexpressing tumor cells. In addition, padnarsertib binds to and inhibits the activity of NAMPT. This depletes cellular NAD and inhibits NAD-dependent enzymes, both of which are needed for rapid cell proliferation; this results in tumor cell death in NAMPT-overexpressing cancer cells. PAK4, a serine/threonine kinase and member of the PAK family of proteins upregulated in various cancer cell types, regulates cell motility, proliferation and survival. NAMPT, an enzyme that is responsible for maintaining the intracellular NAD pool, plays a key role in the regulation of cellular metabolism and has cytokine-like activities. NAMPT is often overexpressed in a variety of cancers and metabolic disorders and tumor cells rely on NAMPT activity for their NAD supply.

Kpt 9274 Manufacturers

A Kpt 9274 manufacturer is defined as any person or entity involved in the manufacture, preparation, processing, compounding or propagation of Kpt 9274, including repackagers and relabelers. The FDA regulates Kpt 9274 manufacturers to ensure that their products comply with relevant laws and regulations and are safe and effective to use. Kpt 9274 API Manufacturers are required to adhere to Good Manufacturing Practices (GMP) to ensure that their products are consistently manufactured to meet established quality criteria.

Kpt 9274 Suppliers

A Kpt 9274 supplier is an individual or a company that provides Kpt 9274 active pharmaceutical ingredient (API) or Kpt 9274 finished formulations upon request. The Kpt 9274 suppliers may include Kpt 9274 API manufacturers, exporters, distributors and traders.

Kpt 9274 GMP

Kpt 9274 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 Kpt 9274 GMP manufacturers, exporters & distributors, which can be sorted by USDMF, JDMF, KDMF, CEP (COS), WC, API price, and more, enabling you to easily find the right Kpt 9274 GMP manufacturer or Kpt 9274 GMP API supplier for your needs.

Kpt 9274 CoA

A Kpt 9274 CoA (Certificate of Analysis) is a formal document that attests to Kpt 9274's compliance with Kpt 9274 specifications and serves as a tool for batch-level quality control.

Kpt 9274 CoA mostly includes findings from lab analyses of a specific batch. For each Kpt 9274 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.

Kpt 9274 may be tested according to a variety of international standards, such as European Pharmacopoeia (Kpt 9274 EP), Kpt 9274 JP (Japanese Pharmacopeia) and the US Pharmacopoeia (Kpt 9274 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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