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Chemical Structure| 336113-53-2 Chemical Structure| 336113-53-2

Structure of Ispinesib
CAS No.: 336113-53-2

Chemical Structure| 336113-53-2

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Ispinesib is a quinazolinone-derived, specific and reversible kinesin spindle protein inhibitor with Kiapp value of 1.7 nM.

Synonyms: SB-715992; CK0238273

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Product Details of Ispinesib

CAS No. :336113-53-2
Formula : C30H33ClN4O2
M.W : 517.06
SMILES Code : O=C(N(CCCN)[C@@H](C(N1CC2=CC=CC=C2)=NC3=C(C=CC(Cl)=C3)C1=O)C(C)C)C4=CC=C(C)C=C4
Synonyms :
SB-715992; CK0238273
MDL No. :MFCD22628831
InChI Key :QJZRFPJCWMNVAV-HHHXNRCGSA-N
Pubchem ID :6851740

Safety of Ispinesib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Ispinesib

cytoskeleton

Isoform Comparison

Biological Activity

Target
  • Kinesin

    KSP (HsEg5), Ki app:1.7 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
K562 cells 100 nM To assess the inhibitory effects on cancer cell lines. PMC3428805
HeLa cells 1 nM 72 hours To evaluate the inhibitory effect of Ispinesib on HeLa cell proliferation, results showed that Ispinesib synergistically inhibited cell proliferation with KIF15-IN-1. PMC5960320
HCT116 cells 50 – 125 nM two to four weeks To select resistant clones and analyze their resistance mechanisms PMC4123312
HeLa cells 10 nM to 100 nM 10 days To validate the A133P mutation's resistance to Ispinesib via CRISPR/Cas9 genome editing PMC4123312
MDA-MB-468 cells 150 mM 48 hours To evaluate the cell cycle and apoptotic responses of MDA-MB-468 cells to Ispinesib, results showed cell cycle arrest at M phase and induction of apoptosis. PMC2844774
BT-474 cells 150 mM 48 hours To evaluate the cell cycle and apoptotic responses of BT-474 cells to Ispinesib, results showed transient cell cycle arrest at M phase followed by re-entry into interphase. PMC2844774

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Breast cancer xenograft models Intraperitoneal injection 10 mg/kg or 8 mg/kg Every 4 days for 3 doses To evaluate the antitumor activity of Ispinesib in breast cancer xenograft models, results showed tumor regression in all models, with complete regression in some models. PMC2844774

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00169520 Solid Tumor Cancer Phase 1 Completed - United Kingdom ... More >> GSK Investigational Site Oxford, Oxfordshire, United Kingdom, OX2 6PD GSK Investigational Site London, United Kingdom, SW3 6JJ Less <<
NCT00607841 Breast Neoplasms Phase 1 Phase 2 Completed - Peru ... More >> Hospital Nacional Alberto Sabogal Sologúren Lima, Peru Hospital Nacional Edgardo Rebagliati Martins Lima, Peru Instituto Nacional de Enfermedades Neoplásicas Lima, Peru Less <<
NCT00103311 - Completed - -
NCT00103311 Recurrent Colon Cancer ... More >> Recurrent Rectal Cancer Stage IIIA Colon Cancer Stage IIIA Rectal Cancer Stage IIIB Colon Cancer Stage IIIB Rectal Cancer Stage IIIC Colon Cancer Stage IIIC Rectal Cancer Stage IVA Colon Cancer Stage IVA Rectal Cancer Stage IVB Colon Cancer Stage IVB Rectal Cancer Less << Phase 2 Completed - United States, California ... More >> University of Southern California, Norris Los Angeles, California, United States, 90033 Less <<
NCT00085813 Non-Small-Cell Lung Cancer PHASE2 COMPLETED 2025-10-05 GSK Investigational Site, Scot... More >>tsdale, Arizona, 85259, United States|GSK Investigational Site, Jacksonville, Florida, 32224, United States|GSK Investigational Site, Rochester, Minnesota, 55905, United States|GSK Investigational Site, Rochester, New York, 14623, United States|GSK Investigational Site, Greensboro, North Carolina, 27403, United States|GSK Investigational Site, Philadelphia, Pennsylvania, 19111, United States|GSK Investigational Site, Memphis, Tennessee, 38104, United States|GSK Investigational Site, Bruxelles, 1000, Belgium|GSK Investigational Site, Edegem, 2650, Belgium|GSK Investigational Site, Leuven, 3000, Belgium|GSK Investigational Site, Sutton, Surrey, SM2 5PT, United Kingdom Less <<
NCT00095953 Melanoma (Skin) Phase 2 Completed - Canada, British Columbia ... More >> British Columbia Cancer Agency - Centre for the Southern Interior Kelowna, British Columbia, Canada, V1Y 5L3 Fraser Valley Cancer Centre at British Columbia Cancer Agency Surrey, British Columbia, Canada, V3V 1Z2 British Columbia Cancer Agency - Vancouver Cancer Centre Vancouver, British Columbia, Canada, V5Z 4E6 Canada, Nova Scotia Nova Scotia Cancer Centre at Queen Elizabeth II Health Sciences Centre Halifax, Nova Scotia, Canada, B3H 1V7 Canada, Ontario Margaret and Charles Juravinski Cancer Centre Hamilton, Ontario, Canada, L8V 5C2 Toronto Sunnybrook Regional Cancer Centre at Sunnybrook and Women's College Health Sciences Centre Toronto, Ontario, Canada, M4N 3M5 Canada, Quebec Centre Hospitalier de l'Universite de Montreal Montreal, Quebec, Canada, H2L-4M1 Less <<
NCT00101244 Adult Grade III Lymphomatoid G... More >>ranulomatosis Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue Nodal Marginal Zone B-cell Lymphoma Recurrent Adult Burkitt Lymphoma Recurrent Adult Diffuse Large Cell Lymphoma Recurrent Adult Diffuse Mixed Cell Lymphoma Recurrent Adult Diffuse Small Cleaved Cell Lymphoma Recurrent Adult Grade III Lymphomatoid Granulomatosis Recurrent Adult Hodgkin Lymphoma Recurrent Adult Immunoblastic Large Cell Lymphoma Recurrent Adult Lymphoblastic Lymphoma Recurrent Grade 1 Follicular Lymphoma Recurrent Grade 2 Follicular Lymphoma Recurrent Grade 3 Follicular Lymphoma Recurrent Mantle Cell Lymphoma Recurrent Marginal Zone Lymphoma Recurrent Small Lymphocytic Lymphoma Splenic Marginal Zone Lymphoma Stage IV Adult Burkitt Lymphoma Stage IV Adult Diffuse Large Cell Lymphoma Stage IV Adult Diffuse Mixed Cell Lymphoma Stage IV Adult Diffuse Small Cleaved Cell Lymphoma Stage IV Adult Hodgkin Lymphoma Stage IV Adult Immunoblastic Large Cell Lymphoma Stage IV Adult Lymphoblastic Lymphoma Stage IV Grade 1 Follicular Lymphoma Stage IV Grade 2 Follicular Lymphoma Stage IV Grade 3 Follicular Lymphoma Stage IV Mantle Cell Lymphoma Stage IV Marginal Zone Lymphoma Stage IV Small Lymphocytic Lymphoma Unspecified Adult Solid Tumor, Protocol Specific Waldenstr?m Macroglobulinemia Less << Phase 1 Terminated(Administratively Co... More >>mplete.) Less << - United States, Michigan ... More >> Barbara Ann Karmanos Cancer Institute Detroit, Michigan, United States, 48201 Less <<
NCT00096499 Adenocarcinoma of the Prostate... More >> Recurrent Prostate Cancer Stage IV Prostate Cancer Less << Phase 2 Completed - United States, Texas ... More >> Southwest Oncology Group San Antonio, Texas, United States, 78245 Less <<
NCT00097409 Ovarian Cancer PHASE2 COMPLETED 2025-05-07 GSK Investigational Site, Birm... More >>ingham, Alabama, 35205, United States|GSK Investigational Site, New Orleans, Louisiana, 70115, United States|GSK Investigational Site, St. Louis, Missouri, 63110, United States|GSK Investigational Site, Mayfield Heights, Ohio, 44124, United States|GSK Investigational Site, Oklahoma City, Oklahoma, 73104, United States|GSK Investigational Site, Abington, Pennsylvania, 19001-3788, United States|GSK Investigational Site, Nashville, Tennessee, 37203, United States|GSK Investigational Site, Seattle, Washington, 98101, United States|GSK Investigational Site, Madison, Wisconsin, 53792, United States Less <<
NCT00095992 Liver Cancer Phase 2 Completed - Canada, British Columbia ... More >> BCCA - Vancouver Cancer Centre Vancouver, British Columbia, Canada, V5Z 4E6 Canada, Ontario Juravinski Cancer Centre at Hamilton Health Sciences Hamilton, Ontario, Canada, L8V 5C2 Cancer Centre of Southeastern Ontario at Kingston Kingston, Ontario, Canada, K7L 5P9 Univ. Health Network-Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 Less <<
NCT00136578 Solid Tumours Phase 1 Completed - United States, Tennessee ... More >> GSK Investigational Site Nashville, Tennessee, United States, 37203 United Kingdom GSK Investigational Site Newcastle Upon Tyne, Northumberland, United Kingdom, NE4 6BE Less <<
NCT00098826 Acute Undifferentiated Leukemi... More >>a Adult Acute Megakaryoblastic Leukemia (M7) Adult Acute Minimally Differentiated Myeloid Leukemia (M0) Adult Acute Monoblastic Leukemia (M5a) Adult Acute Monocytic Leukemia (M5b) Adult Acute Myeloblastic Leukemia With Maturation (M2) Adult Acute Myeloblastic Leukemia Without Maturation (M1) Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities Adult Acute Myeloid Leukemia With Inv(16)(p13;q22) Adult Acute Myeloid Leukemia With t(15;17)(q22;q12) Adult Acute Myeloid Leukemia With t(16;16)(p13;q22) Adult Acute Myeloid Leukemia With t(8;21)(q22;q22) Adult Acute Myelomonocytic Leukemia (M4) Adult Acute Promyelocytic Leukemia (M3) Adult Erythroleukemia (M6a) Adult Pure Erythroid Leukemia (M6b) Blastic Phase Chronic Myelogenous Leukemia de Novo Myelodysplastic Syndromes Previously Treated Myelodysplastic Syndromes Recurrent Adult Acute Lymphoblastic Leukemia Recurrent Adult Acute Myeloid Leukemia Refractory Anemia With Excess Blasts Refractory Anemia With Excess Blasts in Transformation Relapsing Chronic Myelogenous Leukemia Secondary Acute Myeloid Leukemia Secondary Myelodysplastic Syndromes Untreated Adult Acute Myeloid Leukemia Less << Phase 1 Completed - United States, Ohio ... More >> Case Western Reserve University Cleveland, Ohio, United States, 44106 Less <<
NCT00363272 Childhood Burkitt Lymphoma ... More >> Childhood Central Nervous System Germ Cell Tumor Childhood Choroid Plexus Tumor Childhood Craniopharyngioma Childhood Grade I Meningioma Childhood Grade II Meningioma Childhood Grade III Meningioma Childhood High-grade Cerebral Astrocytoma Childhood Infratentorial Ependymoma Childhood Low-grade Cerebral Astrocytoma Childhood Spinal Cord Neoplasm Childhood Supratentorial Ependymoma Recurrent Childhood Brain Stem Glioma Recurrent Childhood Brain Tumor Recurrent Childhood Cerebellar Astrocytoma Recurrent Childhood Cerebral Astrocytoma Recurrent Childhood Ependymoma Recurrent Childhood Grade III Lymphomatoid Granulomatosis Recurrent Childhood Large Cell Lymphoma Recurrent Childhood Lymphoblastic Lymphoma Recurrent Childhood Medulloblastoma Recurrent Childhood Small Noncleaved Cell Lymphoma Recurrent Childhood Supratentorial Primitive Neuroectodermal Tumor Recurrent Childhood Visual Pathway and Hypothalamic Glioma Unspecified Childhood Solid Tumor, Protocol Specific Less << Phase 1 Completed - United States, California ... More >> Children's Oncology Group Arcadia, California, United States, 91006-3776 Less <<
NCT00095628 Metastatic Squamous Neck Cance... More >>r With Occult Primary Squamous Cell Carcinoma Recurrent Metastatic Squamous Neck Cancer With Occult Primary Recurrent Salivary Gland Cancer Recurrent Squamous Cell Carcinoma of the Hypopharynx Recurrent Squamous Cell Carcinoma of the Larynx Recurrent Squamous Cell Carcinoma of the Lip and Oral Cavity Recurrent Squamous Cell Carcinoma of the Oropharynx Recurrent Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity Recurrent Verrucous Carcinoma of the Larynx Recurrent Verrucous Carcinoma of the Oral Cavity Stage IV Squamous Cell Carcinoma of the Hypopharynx Stage IV Squamous Cell Carcinoma of the Larynx Stage IV Squamous Cell Carcinoma of the Lip and Oral Cavity Stage IV Squamous Cell Carcinoma of the Oropharynx Stage IV Verrucous Carcinoma of the Larynx Stage IV Verrucous Carcinoma of the Oral Cavity Stage IVA Salivary Gland Cancer Stage IVA Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity Stage IVB Salivary Gland Cancer Stage IVB Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity Stage IVC Salivary Gland Cancer Stage IVC Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity Less << Phase 2 Completed - Canada, Ontario ... More >> Princess Margaret Hospital Phase 2 Consortium Toronto, Ontario, Canada, M5G 2M9 Less <<
NCT00095628 - Completed - -
NCT00089973 Neoplasms, Breast PHASE2 COMPLETED 2006-08-25 GSK Investigational Site, Jack... More >>sonville, Florida, 32224, United States|GSK Investigational Site, Indianapolis, Indiana, 46202, United States|GSK Investigational Site, Chapel Hill, North Carolina, 27599, United States|GSK Investigational Site, Pittsburgh, Pennsylvania, 15213, United States|GSK Investigational Site, Bruxelles, 1000, Belgium|GSK Investigational Site, Bandar Tun Razak, Cheras, 56000, Malaysia|GSK Investigational Site, Bandar Tun Razak, Cheras, 59100, Malaysia|GSK Investigational Site, Singapore, 119074, Singapore|GSK Investigational Site, Singapore, 169610, Singapore|GSK Investigational Site, Southampton, Hampshire, SO16 6YD, United Kingdom|GSK Investigational Site, Manchester, Lancashire, M20 4BX, United Kingdom|GSK Investigational Site, Newcastle Upon Tyne, Northumberland, NE4 6BE, United Kingdom|GSK Investigational Site, London, W12 0NN, United Kingdom Less <<
NCT00119171 Solid Tumor Cancer Phase 1 Completed - United States, Texas ... More >> GSK Investigational Site San Antonio, Texas, United States, 78229 Less <<
NCT00089973 Neoplasms, Breast PHASE2 COMPLETED 2006-08-25 GSK Investigational Site, Jack... More >>sonville, Florida, 32224, United States|GSK Investigational Site, Indianapolis, Indiana, 46202, United States|GSK Investigational Site, Chapel Hill, North Carolina, 27599, United States|GSK Investigational Site, Pittsburgh, Pennsylvania, 15213, United States|GSK Investigational Site, Bruxelles, 1000, Belgium|GSK Investigational Site, Bandar Tun Razak, Cheras, 56000, Malaysia|GSK Investigational Site, Bandar Tun Razak, Cheras, 59100, Malaysia|GSK Investigational Site, Singapore, 119074, Singapore|GSK Investigational Site, Singapore, 169610, Singapore|GSK Investigational Site, Southampton, Hampshire, SO16 6YD, United Kingdom|GSK Investigational Site, Manchester, Lancashire, M20 4BX, United Kingdom|GSK Investigational Site, Newcastle Upon Tyne, Northumberland, NE4 6BE, United Kingdom|GSK Investigational Site, London, W12 0NN, United Kingdom Less <<
NCT00354250 Recurrent Renal Cell Cancer ... More >> Stage III Renal Cell Cancer Stage IV Renal Cell Cancer Less << Phase 2 Completed - United States, Illinois ... More >> University of Chicago Comprehensive Cancer Center Chicago, Illinois, United States, 60637-1470 Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.93mL

0.39mL

0.19mL

9.67mL

1.93mL

0.97mL

19.34mL

3.87mL

1.93mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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