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Chemical Structure| 895158-95-9 Chemical Structure| 895158-95-9

Structure of SC144
CAS No.: 895158-95-9

Chemical Structure| 895158-95-9

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SC144 showed its function through both exhibiting potent cytotoxicity, by itself or synergism with other compounds, against a panel of drug-sensitive and drug-resistant cancer cell lines, and targeting to gp130.

Synonyms: SC144

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Product Details of SC144

CAS No. :895158-95-9
Formula : C16H11FN6O
M.W : 322.30
SMILES Code : O=C(C1=NC=CN=C1)NNC2=NC3=C(N4C2=CC=C4)C=CC(F)=C3
Synonyms :
SC144
MDL No. :MFCD25976763
InChI Key :UEADAWQSJOWXBK-UHFFFAOYSA-N
Pubchem ID :400169

Safety of SC144

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

Related Pathways of SC144

TLR

Isoform Comparison

Biological Activity

Target
  • P-gp

In Vitro:

Cell Line
Concentration Treated Time Description References
3T3-L1 preadipocytes 10 µM 24 hours Inhibition of ATX expression in adipocytes J Lipid Res. 2017 Nov;58(11):2102-2113
C6 glioma cells 20 µM 1 hour Inhibits IL-6 signaling pathway, reduces sCp gene expression in C6 glioma cells Cell Commun Signal. 2014 Oct 14;12:65
CD34+ cells from CALR-mutated patients 4.3 ± 0.2 nM (IC50) 12 days Inhibited CFU-Mk colony formation, IC50 of 4.3 ± 0.2 nM Blood Adv. 2021 Apr 27;5(8):2184-2195
SK-OV-3 cells 1.2 µM 2 hours To measure hypoxia levels induced by SC144, results showed increased nitroreductase activity Theranostics. 2020 May 25;10(15):6959-6976
4T1 cells 10 µM 24 hours SC144 induced apoptosis and immunogenic cell death (ICD) of 4T1 cells, characterized by upregulation of calreticulin (CRT). Nat Commun. 2023 Aug 8;14(1):4771
MC38 cells 10 µM 24 hours SC144 induced apoptosis and immunogenic cell death (ICD) of MC38 cells, characterized by increased secretion of HMGB-1 and CXCL-10 and upregulation of calreticulin (CRT). Nat Commun. 2023 Aug 8;14(1):4771
Bone marrow-derived macrophages (BMDM) 10 µM 24 hours SC144 treatment increased the frequency of CD206lowMHCIIhighM1-like macrophages and decreased CD206highMHCIIlowM2-like macrophages, indicating polarization of macrophages toward M1 phenotype. Nat Commun. 2023 Aug 8;14(1):4771
E8 0.05-1 µM 24-48 hours SC144 significantly inhibited the growth and viability of E8 cells and reduced the expression of survivin. Br J Cancer. 2015 Jul 14;113(2):242-51
CE2 0.05-1 µM 24-48 hours SC144 significantly inhibited the growth and viability of CE2 cells and reduced the expression of survivin. Br J Cancer. 2015 Jul 14;113(2):242-51
CE1 0.05-1 µM 24-48 hours SC144 significantly inhibited the growth and viability of CE1 cells and reduced the expression of survivin. Br J Cancer. 2015 Jul 14;113(2):242-51
C4-2B 0.05-1 µM 24-48 hours SC144 significantly inhibited the growth and viability of C4-2B cells and reduced the expression of survivin. Br J Cancer. 2015 Jul 14;113(2):242-51
DU145 0.05-1 µM 24-48 hours SC144 significantly inhibited the growth and viability of DU145 cells and reduced the expression of survivin. Br J Cancer. 2015 Jul 14;113(2):242-51
PC3 0.05-1 µM 24-48 hours SC144 significantly inhibited the growth and viability of PC3 cells and reduced the expression of survivin. Br J Cancer. 2015 Jul 14;113(2):242-51
LNCaP 0.05-1 µM 24-48 hours SC144 significantly inhibited the growth and viability of LNCaP cells and reduced the expression of survivin and MMP-9. Br J Cancer. 2015 Jul 14;113(2):242-51
CD8+ T-cells 2 µM 24-72 hours SC144 exhibited cytotoxicity among activated CD8+ T-cells, leading to reduced cell numbers. Nat Commun. 2023 Aug 8;14(1):4771
UT7 cells 5 µM 3 days Inhibited proliferation of CALR DEL and KO UT7 cells, reducing by 63.9% ± 3% and 50% ± 4.1% Blood Adv. 2021 Apr 27;5(8):2184-2195
UT7/mpl cells 5 µM 3 days Inhibited proliferation of CALR DEL and KO UT7/mpl cells, reducing by 58.3% ± 1.2% and 57.2% ± 3.6% Blood Adv. 2021 Apr 27;5(8):2184-2195
LNCaP cells 2 µM 4 hours To validate transcriptional effects of SC144 in an independent cell line, results showed upregulation of HIF1A-AS2 transcription Theranostics. 2020 May 25;10(15):6959-6976
OVCAR-8 cells 1.2 µM 4 hours To assess the effect of SC144 on hypoxia-related gene transcription, results showed upregulation of HIF1A-AS2 transcription Theranostics. 2020 May 25;10(15):6959-6976
ASPC cells 1, 2 µM 48 hours To evaluate the effect of SC144 on ASPC cell viability and proliferation. Results showed that 1 and 2 µM SC144 alone significantly inhibited the viability of ASPC cells (p < 0.001). Paclitaxel did not further enhance the effects observed with single SC144 treatment. Cancers (Basel). 2023 Jan 11;15(2):456
L3.6pl cells 0.1, 0.2, 1, 2 µM 48 hours To evaluate the effect of SC144 on cell viability and proliferation. Results showed that 1 and 2 µM SC144 alone significantly inhibited the viability of L3.6pl cells (p < 0.01, p < 0.001). However, combined treatment with 0.1, 0.2, and 1 µM SC144 blocked the effect of 10 nM paclitaxel on viability reduction. Cancers (Basel). 2023 Jan 11;15(2):456

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats Monocrotaline (MCT)-induced pulmonary arterial hypertension model Intraperitoneal injection 10 mg/kg Daily injection, duration not specified SC144 improved right ventricular function, reduced right ventricular macrophage count, and suppressed NLRP3 inflammasome and STAT3 activation. Am J Respir Crit Care Med. 2022 Sep 1;206(5):608-624
C57BL/6 mice High-fat diet-induced obese mouse model Oral 10 mg/kg Once daily for one week Suppressed ATX expression in adipose tissue, decreased plasma ATX and LPA levels, and improved insulin sensitivity and glucose tolerance in high-fat diet-fed obese mice J Lipid Res. 2017 Nov;58(11):2102-2113
Sprague Dawley rats MCT-induced pulmonary arterial hypertension model Intraperitoneal injection 10 mg/kg Once daily for 10 days SC144 decreased GP130 activation, which normalized MT-JPH2 protein expression and t-tubule structure in the MCT RV. SC144 also reduced RV hypertrophy and fibrosis and augmented RV-pulmonary artery coupling without altering PAH severity. Circ Heart Fail. 2022 Jan;15(1):e008574
BALB/c nu/nu mice Pancreatic ductal adenocarcinoma (PDAC) mouse model Intraperitoneal injection 100 mg/kg SC144 + 10 mg/kg paclitaxel SC144 injected daily, paclitaxel injected every four days, for 26 days To evaluate the effect of SC144/paclitaxel combination therapy on tumor growth in a PDAC mouse model. Results showed that SC144/paclitaxel combination therapy significantly reduced tumor weight and volume (p < 0.05 and p < 0.01). Additionally, SC144/paclitaxel treatment reduced human IL-6 levels in the tumors and plasma of mice (p < 0.05). Cancers (Basel). 2023 Jan 11;15(2):456
C57BL/6 mice MOC2-E6/E7 tumor model Intraperitoneal injection 40 mg/kg Once daily for two weeks To evaluate the antitumor efficacy of SC144, results showed significant reduction in tumor burden Theranostics. 2020 May 25;10(15):6959-6976
C57BL/6 mice MC38 colon carcinoma model Intravenous injection 5 mg/kg Administered on days 11, 13, and 15 SC144@HABN treatment significantly reduced tumor growth, increased the frequency of tumor-infiltrating CD8+ T-cells, and elevated the ratio of M1-like to M2-like macrophages. Nat Commun. 2023 Aug 8;14(1):4771
Mice Experimental AD-like skin inflammation model Intraperitoneal injection 7 mg/kg/day Once daily (weekdays), continued for 3 weeks SC144 treatment significantly inhibited the AD-like symptoms in Ets1ΔdLck mice, characterized by reduced pathophysiology and ear thickness. This was associated with reduced lymphocytes infiltration and reduced serum IgE and IgG level. Moreover, SC144 treatment significantly reduced IL-17A and IL-22 production in CD4+ T cells from the dLNs compared with vehicle controls. JCI Insight. 2019 Mar 7;4(5):e124202

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.10mL

0.62mL

0.31mL

15.51mL

3.10mL

1.55mL

31.03mL

6.21mL

3.10mL

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