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Chemical Structure| 1450833-55-2 Chemical Structure| 1450833-55-2

Structure of TAK-243
CAS No.: 1450833-55-2

Chemical Structure| 1450833-55-2

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TAK-243, also known as MLN7243 and AOB87172, is a small molecule inhibitor of ubiquitin-activating enzyme (UAE), with potential antineoplastic activity.

Synonyms: MLN7243

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Product Details of TAK-243

CAS No. :1450833-55-2
Formula : C19H20F3N5O5S2
M.W : 519.52
SMILES Code : O=S(OC[C@@H]1[C@@H](O)[C@@H](O)[C@H](NC2=CC=NC3=CC(C4=CC=CC(SC(F)(F)F)=C4)=NN23)C1)(N)=O
Synonyms :
MLN7243
MDL No. :MFCD28964160
InChI Key :KJDAGXLMHXUAGV-DGWLBADLSA-N
Pubchem ID :71715374

Safety of TAK-243

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

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Human meningioma cell line (Ben-Men-1) 100 nM 24 hours To evaluate the apoptotic effect of TAK-243 on NF2-deficient meningioma cells, results showed that TAK-243 significantly induced apoptosis. PMC10479743
Human meningioma cell line (MN1-LF) 100 nM 24 hours To evaluate the apoptotic effect of TAK-243 on NF2-deficient meningioma cells, results showed that TAK-243 significantly induced apoptosis. PMC10479743
MDS-L cells 12.5 nM 72 hours To evaluate the effect of TAK-243 in combination with DAC on apoptosis, the results showed that the combination significantly increased the proportion of apoptotic cells. PMC11358161
MOLM-13 cells 12.5 nM 72 hours To evaluate the effect of TAK-243 in combination with DAC on apoptosis, the results showed that the combination significantly increased the proportion of apoptotic cells. PMC11358161
CCRF-CEM SLFN11-WT and SLFN11-KO cells 63.2 nM and 189.6 nM TAK-243 showed greater cytotoxicity in SLFN11-KO cells PMC8178208
DLBCL cells 30 to 180 nM 24 hours induced apoptosis PMC10682029
OCI-LY19 cells 30 nM 24 hours partial G2/M-phase arrest PMC6325297
OCI-LY19 cells 100 nM or higher 24 hours accumulation of cells in both S and M phases PMC6325297
SCLC cell lines 0-1 µmol/L 3 days Evaluate the efficacy of TAK-243 as monotherapy, results showed most SCLC cell lines were sensitive to TAK-243 with a median EC50 of 15.8 nmol/L. PMC9365348
SCLC cell lines 0-2 µmol/L 6 days Evaluate the synergy of TAK-243 with C/E chemotherapy or olaparib, results showed TAK-243 synergized with both C/E and olaparib in vitro. PMC9365348

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mouse NF2-deficient meningioma xenograft model Intraperitoneal injection 10 mg/kg once every 3 days, for 8 weeks To evaluate the anti-tumor effect of TAK-243 on NF2-deficient meningioma xenograft models, results showed that TAK-243 significantly suppressed tumor growth. PMC10479743
mice MOLM-13 xenograft model intraperitoneal injection 30 mg/kg once daily for 15 days To evaluate the effect of TAK-243 in combination with DAC on the survival of mice, the results showed that the combination significantly prolonged the survival of mice. PMC11358161
mice OCI-LY3 xenografted DLBCL tumor model tail vein injection 10 nM In vitro experiment, no in vivo administration restricted tumor growth, reduced cell proliferation, and increased apoptosis PMC6325297
Mice SCLC patient-derived xenograft (PDX) models Intravenous 30 mg/kg Every 2 days, for 22 days Evaluate the efficacy of TAK-243 as monotherapy, results showed SCRX-Lu149 CN and CR PDX models were sensitive to TAK-243, while JHU-LX33 PDX model was resistant. PMC9365348

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02045095 Advanced Malignant Solid Tumor... More >>s Less << PHASE1 TERMINATED 2016-11-09 Boston, Massachusetts, United ... More >>States|Saint Louis, Missouri, United States|Cleveland, Ohio, United States|Philadelphia, Pennsylvania, United States|Charleston, South Carolina, United States|Nashville, Tennessee, United States|San Antonio, Texas, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.92mL

0.38mL

0.19mL

9.62mL

1.92mL

0.96mL

19.25mL

3.85mL

1.92mL

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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