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    Varlitinib

    DIGITAL CONTENT

    PharmaCompass
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    2D Structure
    Also known as: 845272-21-1, Arry-334543, Arry334543, Arry 334543, Arry-543, Aslan-001
    Molecular Formula
    C22H19ClN6O2S
    Molecular Weight
    466.9  g/mol
    InChI Key
    UWXSAYUXVSFDBQ-CYBMUJFWSA-N
    FDA UNII
    846Y8197W1
    Varlitinib is an orally bioavailable inhibitor of the epidermal growth factor receptor family with potential antineoplastic activity. Varlitinib selectively and reversibly binds to both EGFR (ErbB-1) and Her-2/neu (ErbB-2) and prevents their phosphorylation and activation, which may result in inhibition of the associated signal transduction pathways, inhibition of cellular proliferation and cell death. EGFR and Her-2 play important roles in cell proliferation and differentiation and are upregulated in various human tumor cell types. Due to the dual inhibition of both EGFR and Her-2, this agent may be therapeutically more effective than agents that inhibit EGFR or Her-2 alone.
    1 2D Structure

    2D Structure

    2 Identification
    2.1 Computed Descriptors
    2.1.1 IUPAC Name
    4-N-[3-chloro-4-(1,3-thiazol-2-ylmethoxy)phenyl]-6-N-[(4R)-4-methyl-4,5-dihydro-1,3-oxazol-2-yl]quinazoline-4,6-diamine
    2.1.2 InChI
    InChI=1S/C22H19ClN6O2S/c1-13-10-31-22(27-13)29-14-2-4-18-16(8-14)21(26-12-25-18)28-15-3-5-19(17(23)9-15)30-11-20-24-6-7-32-20/h2-9,12-13H,10-11H2,1H3,(H,27,29)(H,25,26,28)/t13-/m1/s1
    2.1.3 InChI Key
    UWXSAYUXVSFDBQ-CYBMUJFWSA-N
    2.1.4 Canonical SMILES
    CC1COC(=N1)NC2=CC3=C(C=C2)N=CN=C3NC4=CC(=C(C=C4)OCC5=NC=CS5)Cl
    2.1.5 Isomeric SMILES
    C[C@@H]1COC(=N1)NC2=CC3=C(C=C2)N=CN=C3NC4=CC(=C(C=C4)OCC5=NC=CS5)Cl
    2.2 Other Identifiers
    2.2.1 UNII
    846Y8197W1
    2.3 Synonyms
    2.3.1 MeSH Synonyms

    1. Arry-334543

    2.3.2 Depositor-Supplied Synonyms

    1. 845272-21-1

    2. Arry-334543

    3. Arry334543

    4. Arry 334543

    5. Arry-543

    6. Aslan-001

    7. Varlitinib (arry334543)

    8. Aslan001

    9. 846y8197w1

    10. Ar-00334543

    11. (r)-n4-(3-chloro-4-(thiazol-2-ylmethoxy)phenyl)-n6-(4-methyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine

    12. 4-n-[3-chloro-4-(1,3-thiazol-2-ylmethoxy)phenyl]-6-n-[(4r)-4-methyl-4,5-dihydro-1,3-oxazol-2-yl]quinazoline-4,6-diamine

    13. N(sup 4)-(3-chloro-4-(thiazol-2-ylmethoxy)phenyl)-n(sup 6)-((4r)-4-methyl-4,5-dihydrooxazol-2- Yl)quinazoline-4,6-diamine

    14. (r)-n4-(3-chloro-4-(thiazol-2-ylmethoxy)phenyl)-n6-(4-methyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine.

    15. Varlitinib [usan]

    16. Varlitinib [usan:inn]

    17. Unii-846y8197w1

    18. Varlitinib Free Base

    19. Varlitinib [inn]

    20. Varlitinib (usan/inn)

    21. Varlitinib [who-dd]

    22. Mls006011274

    23. Gtpl7645

    24. Schembl1384578

    25. Chembl2103842

    26. Dtxsid501025597

    27. Ex-a1005

    28. Vib27221

    29. Bdbm50205268

    30. Nsc764823

    31. Nsc800962

    32. S2755

    33. Zinc13980035

    34. Akos027250815

    35. Ccg-269421

    36. Cs-5222

    37. Db05944

    38. Nsc-764823

    39. Nsc-800962

    40. Ncgc00346724-01

    41. Ncgc00346724-02

    42. Ac-35277

    43. Hy-10530

    44. Smr004703024

    45. Sw219901-1

    46. D09689

    47. A900002

    48. Q27089126

    49. (r)-4-[[3-chloro-4-[(thiazol-2-yl)methoxy]phenyl]amino]-6-[(4-methyl-4,5-dihydrooxazol-2-yl)amino]quinazoline;varlitinib

    50. 4,6-quinazolinediamine, N(sup 4)-(3-chloro-4-(2-thiazolylmethoxy)phenyl)-n(sup 6)-((4r)-4,5- Dihydro-4-methyl-2-oxazolyl)-

    51. 4,6-quinazolinediamine, N(sup 4)-(3-chloro-4-(2-thiazolylmethoxy)phenyl)-n(sup 6)-((4r)-4,5-dihydro-4-methyl-2-oxazolyl)-

    52. 4,6-quinazolinediamine, N4-(3-chloro-4-(2-thiazolylmethoxy)phenyl)-n6-((4r)-4,5-dihydro-4-methyl-2-oxazolyl)-

    53. N4-(3-chloro-4-(1,3-thiazol-2-ylmethoxy)phenyl)-n6-((4r)-4-methyl-4,5-dihydro-1,3-oxazol-2-yl)quinazoline-4,6-diamine

    2.4 Create Date
    2009-07-20
    3 Chemical and Physical Properties
    Molecular Weight 466.9 g/mol
    Molecular Formula C22H19ClN6O2S
    XLogP34.2
    Hydrogen Bond Donor Count2
    Hydrogen Bond Acceptor Count8
    Rotatable Bond Count7
    Exact Mass466.0978727 g/mol
    Monoisotopic Mass466.0978727 g/mol
    Topological Polar Surface Area122 Ų
    Heavy Atom Count32
    Formal Charge0
    Complexity660
    Isotope Atom Count0
    Defined Atom Stereocenter Count1
    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).

    5 Pharmacology and Biochemistry
    5.1 Mechanism of Action

    Varlitinib is an orally active, reversible, enzymatic and cellular inhibitor, with nanomolar potency, of the key growth factor receptor tyrosine kinases ErbB-2 and EGFR. The compound possesses improved physiochemical properties relative to compounds directed at these targets currently in clinical development, and provides superior exposure and equivalent or greater efficacy in animal models of human cancer. Currently, there is no single drug on the market that selectively inhibits both ErbB-2 and EGFR. Varlitinib, which concurrently inhibits the molecular targets of the drugs Herceptin(R) (ErbB-2) and Erbitux(R) (EGFR), may provide enhanced efficacy in the treatment of cancer patients.