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Chemical Structure| 1400989-25-4 Chemical Structure| 1400989-25-4

Structure of SC-43
CAS No.: 1400989-25-4

Chemical Structure| 1400989-25-4

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SC-43 is an src-homology protein tyrosine phosphatase-1 (SHP-1) agonist which reduces liver fibrosis.

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Product Details of SC-43

CAS No. :1400989-25-4
Formula : C21H13ClF3N3O2
M.W : 431.80
SMILES Code : O=C(NC1=CC=CC(OC2=CC=C(C#N)C=C2)=C1)NC3=CC=C(Cl)C(C(F)(F)F)=C3
MDL No. :MFCD31380911
InChI Key :QIBWSQJZKMUZAK-UHFFFAOYSA-N
Pubchem ID :70688629

Safety of SC-43

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P264-P270-P271-P280-P301+P312-P302+P352-P304+P340-P305+P351+P338-P330-P332+P313-P337+P313-P362-P403+P233-P405-P501

Isoform Comparison

Biological Activity

Description
SC-43, a derivative of Sorafenib, functions as a potent and orally active agonist of SHP-1 (PTPN6). It suppresses the phosphorylation of STAT3 and triggers apoptosis in cells. SC-43 also exhibits anti-fibrotic and anticancer properties[1][2].

In Vitro:

Cell Line
Concentration Treated Time Description References
LX2 cells 2.5 and 5 µM 24 hours SC-43 significantly reduced the viability of LX2 cells and induced apoptosis through STAT3 pathway inhibition Sci Rep. 2017 May 11;7(1):1728
HSC-T6 cells 2.5 and 5 µM 24 hours SC-43 significantly reduced the viability of HSC-T6 cells and induced apoptosis through STAT3 pathway inhibition Sci Rep. 2017 May 11;7(1):1728
SW480 0.5, 1, 5, 10 µM 24 hours SC-43 significantly increased SHP-1 activity, downregulated p-STAT3Tyr705 level, and induced apoptosis in CRC cells Neoplasia. 2015 Sep;17(9):687-696
Hct-15 0.5, 1, 5, 10 µM 24 hours SC-43 significantly increased SHP-1 activity, downregulated p-STAT3Tyr705 level, and induced apoptosis in CRC cells Neoplasia. 2015 Sep;17(9):687-696
HT-29 0.5, 1, 5, 10 µM 24 hours SC-43 significantly increased SHP-1 activity, downregulated p-STAT3Tyr705 level, and induced apoptosis in CRC cells Neoplasia. 2015 Sep;17(9):687-696
DLD1 0.5, 1, 5, 10 µM 24 hours SC-43 significantly increased SHP-1 activity, downregulated p-STAT3Tyr705 level, and induced apoptosis in CRC cells Neoplasia. 2015 Sep;17(9):687-696
Hct-116 0.5, 1, 5, 10 µM 24 hours SC-43 significantly increased SHP-1 activity, downregulated p-STAT3Tyr705 level, and induced apoptosis in CRC cells Neoplasia. 2015 Sep;17(9):687-696
MDA-MB-468 5 µM 36 hours SC-43 inhibited p-STAT3 by upregulating SHP-1 activity, leading to apoptosis Breast Cancer Res. 2013;15(4):R63
HCC-1937 5-7.5 µM 36 hours SC-43 induced more potent apoptotic activity and suppressed cell proliferation by downregulating p-STAT3 and its downstream proteins cyclin D1 and survivin Breast Cancer Res. 2013;15(4):R63

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Female NCr athymic nude mice MDA-MB-468 xenograft tumor model Oral 10 mg/kg Once daily for 28 days SC-43 significantly inhibited the growth of MDA-MB-468 xenograft tumors, correlating with downregulation of p-STAT3 and enhancement of SHP-1 activity Breast Cancer Res. 2013;15(4):R63
Nude mice Hct-116 xenograft model Oral 10 mg/kg per day Once daily for 25 days SC-43 exerts a more suppressive effect on tumor formation in vivo than regorafenib by targeting SHP-1 –dependent STAT3 inhibition Neoplasia. 2015 Sep;17(9):687-696
C57BL/6JNarl mice CCl4-induced liver fibrosis model Oral gavage 5, 10, or 20 mg/kg 5 days a week for 4 or 8 weeks SC-43 significantly ameliorated liver fibrosis and improved mouse survival Sci Rep. 2017 May 11;7(1):1728

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.32mL

0.46mL

0.23mL

11.58mL

2.32mL

1.16mL

23.16mL

4.63mL

2.32mL

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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