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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
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Inaccessible (Haz class 6.1), International USD 150+
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Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Chemical Structure| 1227637-23-1 Chemical Structure| 1227637-23-1

Structure of Tegatrabetan
CAS No.: 1227637-23-1

Chemical Structure| 1227637-23-1

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beta-Catenin inhibitor BC2059 is efficacious as monotherapy or in combination with proteasome inhibitor bortezomib in multiple myeloma.

Synonyms: BC2059; Tegavivint

4.5 *For Research Use Only !

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Product Details of Tegatrabetan

CAS No. :1227637-23-1
Formula : C28H36N4O6S2
M.W : 588.74
SMILES Code : O=S(C1=CC2=C(C=C1)/C(C3=CC=C(S(=O)(N4C[C@H](C)C[C@H](C)C4)=O)C=C3/C2=N\O)=N\O)(N5C[C@H](C)C[C@H](C)C5)=O
Synonyms :
BC2059; Tegavivint
MDL No. :MFCD32633578
InChI Key :OMWCXCBGEFHCTN-FGYAAKKASA-N
Pubchem ID :46212391

Safety of Tegatrabetan

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H315-H318-H334-H335
Precautionary Statements:P261-P264-P271-P280-P280-P284-P302+P352-P304+P340+P312-P305+P351+P338+P310-P332+P313-P342+P311-P362+P364-P403+P233-P405-P501
Class:9
UN#:3335
Packing Group:

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
LM7 18.0 nM 72 h LM7 cells were sensitive to Tegavivint, and it inhibited the expression of b-catenin and c-Myc PMC6855956
BCPAP cells 100 nM 24 h Tegavivint significantly reversed the impact of CDH4 on tube formation in HUVECs. PMC10894493
HFOB1.19 > 1 µM 72 h HFOB1.19 cells were not sensitive to Tegavivint PMC6855956
TCCC-OS84 21.6 nM 72 h TCCC-OS84 cells were sensitive to Tegavivint, and it inhibited the expression of b-catenin and c-Myc PMC6855956
TCCC-OS63 36.6 nM 72 h TCCC-OS63 cells were sensitive to Tegavivint, and it inhibited the expression of b-catenin and c-Myc PMC6855956
SaOS-2 6.2 nM 72 h SaOS-2 cells were sensitive to Tegavivint, and it inhibited the expression of b-catenin and c-Myc PMC6855956
TPC-1 cells 100 nM 24 h Tegavivint effectively counteracted the pro-migratory and invasive effects of CDH4 on PTC cells. PMC10894493
CD34+ AML blast progenitor cells 20-100 nM 48 h BC2059 dose-dependently induced apoptosis in CD34+ AML blast progenitor cells PMC4456205
MV4-11 cells 20-100 nM 48 h BC2059 induced apoptosis in FLT3-ITD expressing MV4-11 cells PMC4456205
OCI-AML3 cells 20-100 nM 120 h BC2059 dose-dependently inhibited cell proliferation and induced apoptosis PMC4456205
DLBCL cell lines 2-100 nM 24 h Induced DLBCL cell death PMC8561281

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Osteosarcoma PDX model Intraperitoneal injection 50 mg/kg Twice weekly for 4 weeks Tegavivint significantly suppressed PDX tumor growth and reduced lung metastasis PMC6855956
Nude mice Lung metastatic model and tumorigenicity studies Intraperitoneal injections 20 mg/kg Twice weekly for three consecutive weeks per cycle, repeated over two cycles lasting 28 days each Tegavivint significantly impeded tumor formation in CDH4-overexpressing TPC-1 cells and significantly reduced the volume and weight of tumors compared to both control and CDH4-overexpressing groups. PMC10894493
NOD/SCID mice AML xenograft model Tail vein injection 1.0, 5.0, 10.0 mg/kg Twice weekly for 3 weeks BC2059 significantly improved the survival of NOD/SCID mice PMC4456205
NSG mice DLBCL models Tail vein injection 25 mg/kg Every 3 days until the end of the experiment Significantly prolonged survival PMC8561281

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03459469 Desmoid Tumor PHASE1 COMPLETED 2022-05-01 Massachusetts General Hospital... More >>, Boston, Massachusetts, 02114, United States|Dana Farber Cancer Institute, Boston, Massachusetts, 02215, United States|Memorial Sloan Kettering Cancer Center, New York, New York, 10065, United States|The Ohio State University Comprehensive Cancer Center, Columbus, Ohio, 43202, United States|MD Anderson Cancer Center, Houston, Texas, 770030, United States|Seattle Cancer Care Alliance, Seattle, Washington, 98109, United States|Princess Margaret Cancer Center, Toronto, Ontario, Canada Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.70mL

0.34mL

0.17mL

8.49mL

1.70mL

0.85mL

16.99mL

3.40mL

1.70mL

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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