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Chemical Structure| 387867-13-2 Chemical Structure| 387867-13-2
Chemical Structure| 387867-13-2

Tandutinib

CAS No.: 387867-13-2

Tandutinib is an antagonist ofFLT3 with IC50 of 0.22 μM and can also inhibitPDGFR andc-Kit thereby inhibiting cellular proliferation and inducing apoptosis.

Synonyms: MLN518; CT53518; MLN0518, MLN 518, MLN-518, MLN518, NSC726292, NSC 726292, NSC-726292, CT53518, CT-53518, CT 53518, D06005, D-06005, D 06005, Tandutinib

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Cat. No.: A895261 Purity: 99%

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Product Details of Tandutinib

CAS No. :387867-13-2
Formula : C31H42N6O4
M.W : 562.70
SMILES Code : CC(C)OC1=CC=C(C=C1)NC(N2CCN(CC2)C3=NC=NC4=CC(OCCCN5CCCCC5)=C(C=C43)OC)=O
Synonyms :
MLN518; CT53518; MLN0518, MLN 518, MLN-518, MLN518, NSC726292, NSC 726292, NSC-726292, CT53518, CT-53518, CT 53518, D06005, D-06005, D 06005, Tandutinib
InChI Key :UXXQOJXBIDBUAC-UHFFFAOYSA-N
Pubchem ID :3038522

Safety of Tandutinib

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

Related Pathways of Tandutinib

RTK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description Reference
HT-29 0–50 µM 24-72 hours Tandutinib significantly inhibited colon cancer cell proliferation PMC4418457
SW480 0–50 µM 24-72 hours Tandutinib significantly inhibited colon cancer cell proliferation PMC4418457
HCT116 0–50 µM 24-72 hours Tandutinib significantly inhibited colon cancer cell proliferation PMC4418457
HEK-MRP7-transfected cells 10 µM 36 and 72 hours To evaluate the effect of Tandutinib on MRP7 protein expression, results showed that Tandutinib did not significantly alter the expression levels of MRP7 protein. PMC3694559
FHC 30 µM 48 hours Tandutinib did not affect normal colonic epithelial cell proliferation PMC4418457
THP-1 cells 100 ng/ml FLT3 ligand 5 and 10 min Activation of FLT3 receptor increases phosphorylation of C/EBPα on S21 PMC2118199
HEK-MRP7-transfected cells 5, 10 µM 72 hours To evaluate the sensitivity of Tandutinib on HEK-MRP7-transfected cells, results showed that Tandutinib did not significantly inhibit cell growth at concentrations up to 10 µM. PMC3694559
HEK293-pcDNA3.1 cells 5, 10 µM 72 hours To evaluate the sensitivity of Tandutinib on HEK293-pcDNA3.1 cells, results showed that Tandutinib did not significantly inhibit cell growth at concentrations up to 10 µM. PMC3694559
AML patient peripheral blood mononuclear cells (PBMCs) 1 μM 72 hours To evaluate the effect of Tandutinib on T cell subsets in AML patient PBMCs, results showed no significant effect on CD4+CD25+ T cell population. PMC6277419
Healthy donor peripheral blood mononuclear cells (PBMCs) 1 μM 72 hours To evaluate the effect of Tandutinib on T cell subsets in healthy donor PBMCs, results showed no significant effect on CD4+CD25+ T cell population. PMC6277419
MonoMac6 cells 1 μM 8 or 24 h Inhibition of FLT3 activity leads to decreased phosphorylation of C/EBPα on S21 PMC2118199
MonoMac1 cells 1 μM 8 or 24 h Inhibition of FLT3 activity leads to decreased phosphorylation of C/EBPα on S21 PMC2118199
MOLM-14 cells 1 μM 8 or 24 h Inhibition of FLT3 activity leads to decreased phosphorylation of C/EBPα on S21 PMC2118199
MOLM-13 cells 1 μM 8 or 24 h Inhibition of FLT3 activity leads to decreased phosphorylation of C/EBPα on S21 PMC2118199
MV4;11 cells 1 μM 8 or 24 h Inhibition of FLT3 activity leads to decreased phosphorylation of C/EBPα on S21 and promotes granulocytic differentiation PMC2118199

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
Athymic nude mice HCT116 colon cancer xenograft model Intraperitoneal injection 50 mg/kg Daily for 21 days Tandutinib significantly suppressed colon cancer xenograft growth and angiogenesis PMC4418457

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00064584 Acute Myelogenous Leukemia|Mye... More >>lodysplastic Syndrome Less << PHASE1 COMPLETED 2025-07-05 UCLA Medical Center, Los Angel... More >>es, California, 90095, United States|Dana Farber Cancer Institute, Boston, Massachusetts, 02115, United States|Memorial Sloan Kettering Cancer Center, New York, New York, 10021, United States|Ohio State University Medical Center, Columbus, Ohio, 43210, United States|Oregon Health Sciences University, Portland, Oregon, 97201, United States Less <<
NCT00274248 Acute Myelogenous Leukemia PHASE1 COMPLETED - The Dana Farber Cancer Institu... More >>te, Boston, Massachusetts, 02134, United States Less <<
NCT00297921 Acute Myelogenous Leukemia Phase 1 Phase 2 Withdrawn - -
NCT00379080 Adult Brain Tumor ... More >> Adult Giant Cell Glioblastoma Adult Glioblastoma Adult Gliosarcoma Recurrent Adult Brain Tumor Less << Phase 1 Phase 2 Completed - United States, Alabama ... More >> University of Alabama at Birmingham Birmingham, Alabama, United States, 35294 United States, Florida H. Lee Moffitt Cancer Center and Research Institute Tampa, Florida, United States, 33612 United States, Georgia Emory University Atlanta, Georgia, United States, 30322 United States, Maryland Johns Hopkins University Baltimore, Maryland, United States, 21287 United States, Massachusetts Massachusetts General Hospital Cancer Center Boston, Massachusetts, United States, 02114 Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 United States, Michigan Henry Ford Hospital Detroit, Michigan, United States, 48202 United States, North Carolina Wake Forest University Health Sciences Winston-Salem, North Carolina, United States, 27157 United States, Ohio Cleveland Clinic Foundation Cleveland, Ohio, United States, 44195 Less <<
NCT00408902 - Completed - -
NCT00667394 Glioblastoma ... More >>Gliosarcoma Anaplastic Astrocytoma Anaplastic Oligodendroglioma Anaplastic Mixed Oligoastrocytoma Less << Phase 2 Completed - United States, Maryland ... More >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 Less <<
NCT00390468 Metastatic Cancer|Pain|Prostat... More >>e Cancer Less << PHASE2 COMPLETED 2025-11-09 M. D. Anderson Cancer Center a... More >>t University of Texas, Houston, Texas, 77030-4009, United States Less <<
NCT00390468 Metastatic Cancer|Pain|Prostat... More >>e Cancer Less << PHASE2 COMPLETED 2025-11-09 M. D. Anderson Cancer Center a... More >>t University of Texas, Houston, Texas, 77030-4009, United States Less <<
NCT00379080 - Completed - -
NCT00408902 Clear Cell Renal Cell Carcinom... More >>a Recurrent Renal Cell Cancer Stage IV Renal Cell Cancer Less << Phase 2 Completed - United States, Ohio ... More >> Case Western Reserve University Cleveland, Ohio, United States, 44106 Less <<
NCT00667394 - Completed - -
NCT00904852 Glioblastoma Multiforme Phase 1 Withdrawn June 2010 -

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.78mL

0.36mL

0.18mL

8.89mL

1.78mL

0.89mL

17.77mL

3.55mL

1.78mL

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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