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Chemistry

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Also known as: 867160-71-2, Osi-906, Linsitinib(osi-906), Osi906, Osi 906, Osi-906aa
Molecular Formula
C26H23N5O
Molecular Weight
421.5  g/mol
InChI Key
PKCDDUHJAFVJJB-UHFFFAOYSA-N
FDA UNII
15A52GPT8T

Linsitinib
Linsitinib is an orally bioavailable small molecule inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. Linsitinib selectively inhibits IGF-1R, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. Overexpressed in a variety of human cancers, IGF-1R stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis.
1 2D Structure

Linsitinib

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
3-[8-amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl]-1-methylcyclobutan-1-ol
2.1.2 InChI
InChI=1S/C26H23N5O/c1-26(32)14-19(15-26)25-30-22(23-24(27)28-11-12-31(23)25)18-8-7-17-9-10-20(29-21(17)13-18)16-5-3-2-4-6-16/h2-13,19,32H,14-15H2,1H3,(H2,27,28)
2.1.3 InChI Key
PKCDDUHJAFVJJB-UHFFFAOYSA-N
2.1.4 Canonical SMILES
CC1(CC(C1)C2=NC(=C3N2C=CN=C3N)C4=CC5=C(C=C4)C=CC(=N5)C6=CC=CC=C6)O
2.2 Other Identifiers
2.2.1 UNII
15A52GPT8T
2.3 Synonyms
2.3.1 MeSH Synonyms

1. 3-(8-amino-1-(2-phenylquinolin-7-yl)imidazo(1,5-a)pyrazin-3-yl)-1-methylcyclobutanol

2. Osi 906

3. Osi-906

4. Osi906

2.3.2 Depositor-Supplied Synonyms

1. 867160-71-2

2. Osi-906

3. Linsitinib(osi-906)

4. Osi906

5. Osi 906

6. Osi-906aa

7. Osi-906 (linsitinib)

8. Asp-7487

9. 3-[8-amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl]-1-methylcyclobutan-1-ol

10. 15a52gpt8t

11. Chembl1091644

12. Mmv676605

13. Cis-3-(8-amino-1-(2-phenyl-7-quinolinyl)imidazo(1,5-a)pyrazin-3-yl)-1-methylcyclobutanol

14. (1r,3r)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl)-1-methylcyclobutanol.

15. Linsitinib [usan]

16. Kinome_3532

17. Linsitinib [usan:inn]

18. Unii-15a52gpt8t

19. Cis-3-(8-amino-1-(2-phenylquinolin-7-yl)imidazo(1,5-a)pyrazin-3-yl)-1-methylcyclobutan-1-ol

20. Cis-3-(8-amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl)-1-methylcyclobutan-1-ol

21. Linsitinib; Osi-906

22. Linsitinib [inn]

23. Linsitinib (usan/inn)

24. Linsitinib (osi-906)

25. Linsitinib [who-dd]

26. Mls006010304

27. Schembl400369

28. Schembl400734

29. Schembl400735

30. Gtpl7423

31. Chembl1996234

32. Schembl10255925

33. Chebi:91402

34. Ex-a719

35. Bcpp000137

36. Bdbm185150

37. Dtxsid401007055

38. Dtxsid901121553

39. Hms3295g15

40. Hms3654c19

41. Bcp01831

42. Bdbm50315887

43. Mfcd12912153

44. Nsc756652

45. Nsc800784

46. S1091

47. Zinc53239527

48. Akos024464740

49. Zinc100071817

50. Zinc113742575

51. Bcp9001035

52. Ccg-264815

53. Cs-0242

54. Db06075

55. Nsc-756652

56. Nsc-800784

57. Pb22643

58. Ncgc00250375-02

59. Ncgc00250375-03

60. Ncgc00250375-11

61. Ncgc00250375-14

62. Ac-26953

63. As-16999

64. Hy-10191

65. Smr004700744

66. Ft-0670821

67. Sw218150-2

68. D09925

69. Sr-05000022538

70. J-520074

71. Q6554803

72. Sr-05000022538-1

73. Brd-k07667918-001-01-3

74. Q27163260

75. 3-[8-amino-1-(2-phenyl-7-quinolinyl)-3-imidazo[1,5-a]pyrazinyl]-1-methyl-1-cyclobutanol

76. (1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl)-1-methylcyclobutanol

77. 1356958-77-4

78. 3-(8-amino-1-(2-phenylquinolin-7-yl)-2,3-dihydroimidazo[1,5-a]pyrazin-3-yl)-1-methylcyclobutanol

79. 3-[8-amino-1-(2-phenyl-quinolin-7-yl)-imidazo[1,5-a]pyrazin-3-yl]-1-methyl-cyclobutanol

80. 867160-72-3

81. Cis-3-(8-amino-1-(2-phenylquinolin-7-yl)imidazo(1,5-a)pyrazin-3-yl)-1-methylcyclobutanol

82. Cyclobutanol, 3-(8-amino-1-(2-phenyl-7-quinolinyl)imidazo(1,5-a)pyrazin-3-yl)-1-methyl-, Cis-

83. Trans-3-[8-amino-1-(2-phenyl-7-quinolinyl)imidazo[1,5-a]pyrazin-3-yl]-1-methylcyclobutanol

2.4 Create Date
2006-10-26
3 Chemical and Physical Properties
Molecular Weight 421.5 g/mol
Molecular Formula C26H23N5O
XLogP34.2
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count5
Rotatable Bond Count3
Exact Mass421.19026037 g/mol
Monoisotopic Mass421.19026037 g/mol
Topological Polar Surface Area89.3 Ų
Heavy Atom Count32
Formal Charge0
Complexity663
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Drug and Medication Information
4.1 Drug Indication

Investigated for use/treatment in cancer/tumors (unspecified) and solid tumors.


5 Pharmacology and Biochemistry
5.1 Pharmacology

In laboratory studies of 28 human tumor cell lines, OSI-906 reduced growth of 15 cell lines representative of colorectal, lung, breast, pancreatic, and pediatric tumors and in mouse models. OSI-906 was particularly effective against tumors that are highly IGF-dependent such as colorectal cancers. According to the researchers, OSI-906 not only slowed tumor growth in mice, but decreased the size of some pre-existing tumors.


5.2 Mechanism of Action

IGF-1R stimulates proliferation, enables onogenic transformation, and suppresses apoptosis. Inhibitors of IGF-1R are expected to have broad utility in oncology since the over-expression of IGF-1R and/or its ligands or the down-regulation of ligand binding proteins occurs in numerous human malignancies including lung, colon, breast, prostate, brain and skin cancers. In addition, signaling through the IGF system has been implicated in protecting tumor cells from apoptosis induced by anti-cancer treatments such as cytotoxic agents and EGFR inhibitors.


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Looking for 867160-71-2 / Linsitinib API manufacturers, exporters & distributors?

Linsitinib manufacturers, exporters & distributors 1

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PharmaCompass offers a list of Linsitinib 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 Linsitinib manufacturer or Linsitinib supplier for your needs.

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

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

API | Excipient name

Linsitinib

Synonyms

867160-71-2, Osi-906, Linsitinib(osi-906), Osi906, Osi 906, Osi-906aa

Cas Number

867160-71-2

Unique Ingredient Identifier (UNII)

15A52GPT8T

About Linsitinib

Linsitinib is an orally bioavailable small molecule inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. Linsitinib selectively inhibits IGF-1R, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. Overexpressed in a variety of human cancers, IGF-1R stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis.

Linsitinib Manufacturers

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

Linsitinib Suppliers

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

Linsitinib GMP

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

Linsitinib CoA

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

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

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