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Chemical Structure| 2097938-73-1 Chemical Structure| 2097938-73-1

Structure of MBQ-167
CAS No.: 2097938-73-1

Chemical Structure| 2097938-73-1

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MBQ-167 is a dual Rac and Cdc42 inhibitor, potential to be developed as an anticancer drug.

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Product Details of MBQ-167

CAS No. :2097938-73-1
Formula : C22H18N4
M.W : 338.41
SMILES Code : CCN1C2=C(C3=C1C=CC=C3)C=C(N4N=NC=C4C5=CC=CC=C5)C=C2
MDL No. :MFCD31746894
InChI Key :LJCANTASZGYJLG-UHFFFAOYSA-N
Pubchem ID :129896932

Safety of MBQ-167

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of MBQ-167

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
BxPC3 cells 0.05 µM 24 h MBQ-167 inhibited the migration rates of RBFOX2-depleted BxPC3 cells without affecting survival or proliferation rates. PMC10156590
KC6141 cells 500 nM 24 h Inhibits CDC42, reduces macropinocytosis, and decreases cell growth PMC8119368
GFP-HER2-BM 62.5 –500 nM 72 h MBQ-167 decreased cell viability of the GFP-HER2-BM cell line and induced apoptosis. PMC10956050
SKBR3-T 250 nM 72 h MBQ-167 inhibited the viability of the SKBR3-T cell line and induced apoptosis. PMC10956050
MDA-MB-231 250 nM 24 h MBQ-167 significantly reduced Rac and Cdc42 activity and led to cell detachment from the substratum. PMC5418092
MCF-7 250 nM 24 h MBQ-167 did not significantly affect the polarity and attachment of MCF-7 cells. PMC5418092
GFP-HER2-BM 250 nM 24 h MBQ-167 significantly inhibited Rac and Cdc42 activity in GFP-HER2-BM cells. PMC5418092
CD45+ cells from Dnmt3a–/– mouse liver 200 nM 20 h To evaluate the effect of MBQ-167 on the migration of CD45+ cells from Dnmt3a–/– mouse liver, results showed that MBQ-167 significantly reduced cell migration. PMC10243813
KPC cells 500 nM 24 h To evaluate the inhibitory effect of MBQ-167 on macropinocytosis, results showed that MBQ-167 inhibited macropinocytosis. PMC9588640
MDA-MB-231 250–500 nM 24 h MBQ-167 treatment reduced colony formation in MDA-MB-231 cells by ~50% in attached cells and ~75% in detached cells. PMC8643341
MDA-MB-468 250 nM 48 h MBQ-167 treatment reduced cell viability in MDA-MB-468 cells by >80%. PMC8643341
4T-1 250 nM 48 h MBQ-167 treatment reduced cell viability in 4T-1 cells by >80%. PMC8643341

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice GFP-labelled RBFOX2-depleted BxPC3 cells or GFP-labelled PDX-derived metastatic X50 cells Intraperitoneal injection 3 mg/kg Every 3 days for a total of 15 doses MBQ-167 inhibited lung metastases without affecting subcutaneous primary tumor growth. PMC10156590
SCID mice GFP-HER2-BM mammary fatpad tumor model intraperitoneal injection 2.5 mg/kg 3 times per week for 8 weeks MBQ-167 significantly inhibited tumor growth and reduced metastasis to lungs and liver. PMC10956050
Nude mice Mammary fatpad tumor model Intraperitoneal injection 1 or 10 mg/kg 3 times a week for 65 days MBQ-167 significantly inhibited mammary tumor growth and metastasis without apparent toxicity. PMC5418092
mice Dnmt3a–/– mice oral 20 mg/kg once daily for 14 days To evaluate the effect of MBQ-167 on Dnmt3a–/– mice, results showed that MBQ-167 significantly reduced hepatosplenomegaly and improved red blood cell, hemoglobin, hematocrit, and platelet levels. PMC10243813
Mice SCID and BALB/c mice Intraperitoneal (IP) and oral 1–10 mg/kg and 5–100 mg/kg 3 times/week (IP) and 5 times/week (oral) for 4 weeks MBQ-167 significantly inhibited tumor growth and lung metastasis in SCID and BALB/c mice, and showed no toxicity in immunocompetent BALB/c mice. PMC8643341

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT06075810 Breast Cancer|Breast Neoplasm|... More >>Breast Cancer Stage IV Less << PHASE1 RECRUITING 2025-10-31 Precision Next Gen Oncology & ... More >>Research Center, Beverly Hills, California, 90212, United States|Florida Cancer Specialists / Sarah Cannon Research Institute / SCRI, Sarasota, Florida, 34232, United States|Sarah Cannon Research Institute/SCRI, Nashville, Tennessee, 37203, United States|FDI Clinical Research, San Juan, 00927, Puerto Rico Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.95mL

0.59mL

0.30mL

14.77mL

2.95mL

1.48mL

29.55mL

5.91mL

2.95mL

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

References

 

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