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Chemical Structure| 1341200-45-0 Chemical Structure| 1341200-45-0

Structure of Dubermatinib
CAS No.: 1341200-45-0

Chemical Structure| 1341200-45-0

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TP-0903 is a selective Axl kinase inhibitor with IC50 of 27 nM.

Synonyms: TP-0903

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Product Details of Dubermatinib

CAS No. :1341200-45-0
Formula : C24H30ClN7O2S
M.W : 516.06
SMILES Code : O=S(C1=CC=CC=C1NC2=NC(NC3=CC=C(CN4CCN(C)CC4)C=C3)=NC=C2Cl)(N(C)C)=O
Synonyms :
TP-0903
MDL No. :MFCD28502172
InChI Key :YUAALFPUEOYPNX-UHFFFAOYSA-N
Pubchem ID :56839178

Safety of Dubermatinib

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

Related Pathways of Dubermatinib

RTK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
H2009 cells 40 nM 72 hours To test the effect of AXL inhibition on cell growth, results showed that AXL inhibition reduced proliferation rates PMC7127959
A549 cells 40 nM 72 hours To test the effect of AXL inhibition on cell growth, results showed that AXL inhibition reduced proliferation rates PMC7127959
U937-derived macrophages 25 ng/mL 72 hours To assess the effect of IL-11 on AXL-STAT3 signaling in macrophages. Results showed that IL-11 treatment significantly increased pSTAT3 levels and AXL expression, and upregulated markers such as CD44. PMC10577802

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nu/J nude mice A549 lung cancer xenograft model Oral 120 mg/kg Twice weekly for 28 days To evaluate the effect of AXL-STAT3 inhibition on tumor growth and macrophage recruitment. Results showed that combination treatment significantly suppressed tumor growth and reduced the recruitment of macrophages and other host cells. PMC10577802

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02729298 Advanced Solid Tumors|EGFR Pos... More >>itive Non-small Cell Lung Cancer|Colorectal Carcinoma|Recurrent Ovarian Carcinoma|BRAF-Mutated Melanoma Less << PHASE1 COMPLETED 2022-06-29 Mayo Clinic Arizona, Phoenix, ... More >>Arizona, 85054, United States|HonorHealth Research Institute, Scottsdale, Arizona, 85258, United States|University of Colorado Denver, Denver, Colorado, 80045, United States|US Oncology - Rocky Mountain Cancer Centers, LLP (RMCC), Denver, Colorado, 80218, United States|Mayo Clinic Florida, Jacksonville, Florida, 32224, United States|Miami Cancer Institute, Miami, Florida, 33176, United States|University of Kansas Cancer Center, Fairway, Kansas, 66205, United States|Mayo Clinic Rochester, Rochester, Minnesota, 55905, United States|US Oncology - Willamette Valley Cancer Institute and Research Center, Eugene, Oregon, 97401, United States|US Oncology - Texas Oncology Austin, Austin, Texas, 78705, United States|University of Texas Southwestern Medical Center, Dallas, Texas, 75390, United States|US Oncology - Texas Oncology - Fort Worth, Fort Worth, Texas, 76104, United States|University of Texas Science Center at San Antonio (UTHSCSA), San Antonio, Texas, 78229, United States|US Oncology - Texas Oncology - Tyler, Tyler, Texas, 75702, United States|US Oncology - Virginia Cancer Specialists (VCS), Fairfax, Virginia, 22031, United States|Medical College of Wisconsin, Milwaukee, Wisconsin, 53226, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.94mL

0.39mL

0.19mL

9.69mL

1.94mL

0.97mL

19.38mL

3.88mL

1.94mL

References

 

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