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Chemistry

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Also known as: 937272-79-2, Pacritinib (sb1518), Sb1518, Sb-1518, Pacritinib(sb1518), Onx-0803
Molecular Formula
C28H32N4O3
Molecular Weight
472.6  g/mol
InChI Key
HWXVIOGONBBTBY-ONEGZZNKSA-N
FDA UNII
G22N65IL3O

Pacritinib
Pacritinib is an orally bioavailable inhibitor of Janus kinase 2 (JAK2), the JAK2 mutant JAK2V617F and FMS-like tyrosine kinase 3 (FLT3; CD135; STK1; FLK2), with potential antineoplastic activity. Upon oral administration, pacritinib competes with JAK2 and the JAK2 mutant JAK2V617F for ATP binding, which may result in inhibition of JAK2 activation, inhibition of the JAK-signal transducer and activator of transcription (STAT) signaling pathway, and the induction of apoptosis. In addition, pacritinib targets, binds to and inhibits the activity of FLT3. This inhibits FLT3-mediated signaling and the proliferation of FLT3-expressing cancer cells. JAK2, often upregulated or mutated in a variety of cancer cells, plays a key role in tumor cell proliferation and survival. The JAK2V617F gain-of-function mutation involves a valine-to-phenylalanine modification at position 617. The JAK-STAT signaling pathway is a major mediator of cytokine activity. FLT3, a class III receptor tyrosine kinase (RTK), is overexpressed or mutated in most B-lineage neoplasms and in acute myeloid leukemias. In addition, JAK2 and FLT3 play a key role in the regulation of the inflammatory response and dendritic cell (DC) proliferation, differentiation and function. Inhibition of JAK2- and FLT3-mediated signaling may suppress the generation and differentiation of DCs, and may regulate inflammatory and immune responses.
Pacritinib is a Kinase Inhibitor. The mechanism of action of pacritinib is as a Tyrosine Kinase Inhibitor, and Janus Kinase Inhibitor, and Cytochrome P450 1A2 Inhibitor, and Cytochrome P450 3A4 Inhibitor, and P-Glycoprotein Inhibitor, and Breast Cancer Resistance Protein Inhibitor, and Organic Cation Transporter 1 Inhibitor.
1 2D Structure

Pacritinib

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
(16E)-11-(2-pyrrolidin-1-ylethoxy)-14,19-dioxa-5,7,27-triazatetracyclo[19.3.1.12,6.18,12]heptacosa-1(24),2(27),3,5,8(26),9,11,16,21(25),22-decaene
2.1.2 InChI
InChI=1S/C28H32N4O3/c1-2-13-32(12-1)14-17-35-27-9-8-25-19-24(27)21-34-16-4-3-15-33-20-22-6-5-7-23(18-22)26-10-11-29-28(30-25)31-26/h3-11,18-19H,1-2,12-17,20-21H2,(H,29,30,31)/b4-3+
2.1.3 InChI Key
HWXVIOGONBBTBY-ONEGZZNKSA-N
2.1.4 Canonical SMILES
C1CCN(C1)CCOC2=C3COCC=CCOCC4=CC(=CC=C4)C5=NC(=NC=C5)NC(=C3)C=C2
2.1.5 Isomeric SMILES
C1CCN(C1)CCOC2=C3COC/C=C/COCC4=CC(=CC=C4)C5=NC(=NC=C5)NC(=C3)C=C2
2.2 Other Identifiers
2.2.1 UNII
G22N65IL3O
2.3 Synonyms
2.3.1 MeSH Synonyms

1. 11-(2-pyrrolidin-1-ylethoxy)-14,19-dioxa-5,7,26-triazatetracyclo(19.3.1.1(2,6).1(8,12))heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene

2. Sb 1518

3. Sb-1518

4. Sb1518

2.3.2 Depositor-Supplied Synonyms

1. 937272-79-2

2. Pacritinib (sb1518)

3. Sb1518

4. Sb-1518

5. Pacritinib(sb1518)

6. Onx-0803

7. Sb 1518

8. G22n65il3o

9. Vonjo

10. 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene

11. 14,19-dioxa-5,7,27-triazatetracyclo(19.3.1.12,6.18,12)heptacosa-1(25),2,4,6(27),8,10,12(26),16,21,23-decaene, 11-(2-(1-pyrrolidinyl)ethoxy)-, (16e)-

12. Chembl2181330

13. Pacritinib [inn]

14. Pacritinib (usan/inn)

15. Pacritinib [usan:inn]

16. Pacritinib [usan]

17. Pacritinib [who-dd]

18. Sb-1518 Tfa Salt

19. Unii-g22n65il3o

20. Gtpl7793

21. Schembl1108221

22. Chembl2035187

23. Schembl22819303

24. Ex-a240

25. Dtxsid801045679

26. Amy23364

27. Bax 2201

28. Bcp09091

29. Onx 0803

30. Bdbm50210177

31. Bdbm50400312

32. Mfcd22572772

33. Nsc759674

34. Nsc781626

35. S8057

36. Akos037515687

37. Ccg-269464

38. Cs-1741

39. Db11697

40. Nsc-759674

41. Nsc-781626

42. Ncgc00381564-02

43. Ncgc00390623-02

44. Ac-30280

45. As-35036

46. Hy-16379

47. Sw219864-1

48. D11768

49. Sb1518;sb-1518;sb 1518

50. Q3888693

51. (16e)-11-(2-pyrrolidin-1-ylethoxy)-14,19-dioxa-5,7,27-triazatetracyclo[19.3.1.12,6.18,12]heptacosa-1(24),2(27),3,5,8(26),9,11,16,21(25),22-decaene

2.4 Create Date
2010-07-06
3 Chemical and Physical Properties
Molecular Weight 472.6 g/mol
Molecular Formula C28H32N4O3
XLogP33.8
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count7
Rotatable Bond Count4
Exact Mass472.24744090 g/mol
Monoisotopic Mass472.24744090 g/mol
Topological Polar Surface Area68.7 Ų
Heavy Atom Count35
Formal Charge0
Complexity644
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count1
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Drug and Medication Information
4.1 Drug Indication

Treatment of post-essential thrombocythaemia myelofibrosis, Treatment of post-polycythaemia vera myelofibrosis


5 Pharmacology and Biochemistry
5.1 FDA Pharmacological Classification
5.1.1 Active Moiety
PACRITINIB
5.1.2 FDA UNII
G22N65IL3O
5.1.3 Pharmacological Classes
Mechanisms of Action [MoA] - Organic Cation Transporter 1 Inhibitors
5.2 ATC Code

L - Antineoplastic and immunomodulating agents

L01 - Antineoplastic agents

L01E - Protein kinase inhibitors

L01EJ - Janus-associated kinase (jak) inhibitors

L01EJ03 - Pacritinib


API SUPPLIERS

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TAPI Technology & API Services

Israel

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

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Virtual BoothTAPI, a leading global supplier of APIs, provides over 350 products and customized CDMO solutions for every stage of development.

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Sun-shine Chem

China

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

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Sun-shine Chem

China

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

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Virtual BoothTAPI, a leading global supplier of APIs, provides over 350 products and customized CDMO solutions for every stage of development.

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Pacritinib

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 with over 350 Products portfolio. 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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Pacritinib

About the Company : Wuhan Sun-shine chemical Corporation Limited (Shanghai Sun-shine Chemical Technology Corporation Limited) is a high-tech enterprise engaged inR&D and sales of related compounds of ...

Wuhan Sun-shine chemical Corporation Limited (Shanghai Sun-shine Chemical Technology Corporation Limited) is a high-tech enterprise engaged inR&D and sales of related compounds of new drugs, specialty pharmaceutical API, advanced intermediates, organic synthetic masonry, and high-end reagents, etc. The special services we provide include: the technical development of chiral drugs, the development of an active molecular library. Sun-shine chemical has over 1,500m² of operation premises. The R&D laboratory is more than 1,000m² and is equipped with a variety of R&D laboratory equipment.
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Pacritinib manufacturers, exporters & distributors 1

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API | Excipient name

Pacritinib

Synonyms

937272-79-2, Pacritinib (sb1518), Sb1518, Sb-1518, Pacritinib(sb1518), Onx-0803

Cas Number

937272-79-2

Unique Ingredient Identifier (UNII)

G22N65IL3O

About Pacritinib

Pacritinib is an orally bioavailable inhibitor of Janus kinase 2 (JAK2), the JAK2 mutant JAK2V617F and FMS-like tyrosine kinase 3 (FLT3; CD135; STK1; FLK2), with potential antineoplastic activity. Upon oral administration, pacritinib competes with JAK2 and the JAK2 mutant JAK2V617F for ATP binding, which may result in inhibition of JAK2 activation, inhibition of the JAK-signal transducer and activator of transcription (STAT) signaling pathway, and the induction of apoptosis. In addition, pacritinib targets, binds to and inhibits the activity of FLT3. This inhibits FLT3-mediated signaling and the proliferation of FLT3-expressing cancer cells. JAK2, often upregulated or mutated in a variety of cancer cells, plays a key role in tumor cell proliferation and survival. The JAK2V617F gain-of-function mutation involves a valine-to-phenylalanine modification at position 617. The JAK-STAT signaling pathway is a major mediator of cytokine activity. FLT3, a class III receptor tyrosine kinase (RTK), is overexpressed or mutated in most B-lineage neoplasms and in acute myeloid leukemias. In addition, JAK2 and FLT3 play a key role in the regulation of the inflammatory response and dendritic cell (DC) proliferation, differentiation and function. Inhibition of JAK2- and FLT3-mediated signaling may suppress the generation and differentiation of DCs, and may regulate inflammatory and immune responses.

Pacritinib Manufacturers

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

click here to find a list of Pacritinib manufacturers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PhamaCompass.

Pacritinib Suppliers

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

click here to find a list of Pacritinib suppliers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PharmaCompass.

Pacritinib GMP

Pacritinib 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 Pacritinib 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 Pacritinib GMP manufacturer or Pacritinib GMP API supplier for your needs.

Pacritinib CoA

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

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

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