SGI-1776 free base
Based on 11 publication(s) in Google Scholar
SGI-1776 free base is an inhibitor of Pim kinases, with IC50s of 7 nM, 363 nM, and 69 nM for Pim-1, -2 and -3, respectively.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.96%
- CAS. Nr.: 1025065-69-3
- Formel: C20H22F3N5O
- Molecular Weight:405.42
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) SGI-1776 free base
More- Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Adv Sci (Weinh). 2025 Jul 6:e03487. [Abstract]
- Cell Death Dis. 2018 Feb 22;9(3):307. [Abstract]
- Phytomedicine. 2026 May 15:157:158301. [Abstract]
- Cell Chem Biol. 2024 Feb 15;31(2):326-337.e11. [Abstract]
- J Med Chem. 2021 Nov 11;64(21):15702-15715. [Abstract]
- Front Cell Infect Microbiol. 2024 Nov 29:14:1502770. [Abstract]
- eNeuro. 2019 Aug 22;6(4):ENEURO.0003-19.2019. [Abstract]
- Anticancer Drugs. 2024 Jan 1;35(1):46-54. [Abstract]
- Patent. US20180263995A1.
Customer Validation & Images
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WB
Biologische Aktivität
Beschreibung
IC50 & Target
Ki: 7 nM (Pim-1), 363 nM (Pim-2), 69 nM (Pim-3)[4]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
<1 μM
Compound: SGI-1776
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Inhibition of human ERG expressed in CHO cells by automated patch clamp method
Inhibition of human ERG expressed in CHO cells by automated patch clamp method
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[PMID: 25589932] |
| HL-60 | GI50 |
1.28 μM
Compound: SGI-1776
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Antiproliferative activity against human HL-60 cells assessed as reduction of cell viability incubated for 72 hrs by trypan blue staining based cell counting analysis
Antiproliferative activity against human HL-60 cells assessed as reduction of cell viability incubated for 72 hrs by trypan blue staining based cell counting analysis
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[PMID: 34515481] |
| K562 | GI50 |
2.19 μM
Compound: SGI-1776
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Antiproliferative activity against human K562 cells assessed as reduction of cell viability incubated for 72 hrs by trypan blue staining based cell counting analysis
Antiproliferative activity against human K562 cells assessed as reduction of cell viability incubated for 72 hrs by trypan blue staining based cell counting analysis
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[PMID: 34515481] |
| K562 | IC50 |
2.29 μM
Compound: 29; SGI-776
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Antiproliferative activity against human K562 cells
Antiproliferative activity against human K562 cells
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[PMID: 34607244] |
| KMS-11 | EC50 |
5 μM
Compound: 1; SGI-1776
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Antiproliferative activity against luciferase expressing human KMS11 cells after 72 hrs by Cell-TiterGlo assay
Antiproliferative activity against luciferase expressing human KMS11 cells after 72 hrs by Cell-TiterGlo assay
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[PMID: 26505898] |
| LNCaP | IC50 |
6.85 μM
Compound: SGI-1776
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Antiproliferative activity against human LNCAP cells after 96 hrs by MTT assay
Antiproliferative activity against human LNCAP cells after 96 hrs by MTT assay
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[PMID: 26804231] |
| MOLM-13 | GI50 |
0.13 μM
Compound: SGI-1776
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Antiproliferative activity against human MOLM13 cells assessed as reduction of cell viability incubated for 72 hrs by trypan blue staining based cell counting analysis
Antiproliferative activity against human MOLM13 cells assessed as reduction of cell viability incubated for 72 hrs by trypan blue staining based cell counting analysis
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[PMID: 34515481] |
| MV4-11 | IC50 |
0.03 μM
Compound: SGI1776
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Growth inhibition of human MV4-11 cells
Growth inhibition of human MV4-11 cells
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[PMID: 29871845] |
| NCI-H1299 | EC50 |
200 nM
Compound: SGI-1776
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Inhibition of PIM1 in human NCI-H1299 cells assessed as reduction in BAD phosphorylation at Ser-112 residue incubated for 4 hrs by ELISA
Inhibition of PIM1 in human NCI-H1299 cells assessed as reduction in BAD phosphorylation at Ser-112 residue incubated for 4 hrs by ELISA
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[PMID: 30802730] |
| PC-3 | GI50 |
4.86 μM
Compound: SGI-1776
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Antiproliferative activity against human PC3 cells after 96 hrs by MTT assay
Antiproliferative activity against human PC3 cells after 96 hrs by MTT assay
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[PMID: 26979485] |
| PC-3 | IC50 |
4.83 μM
Compound: 29; SGI-776
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Antiproliferative activity against human PC-3 cells
Antiproliferative activity against human PC-3 cells
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[PMID: 34607244] |
| PC-3 | IC50 |
4.86 μM
Compound: SGI-1776
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Antiproliferative activity against human PC3 cells after 96 hrs by MTT assay
Antiproliferative activity against human PC3 cells after 96 hrs by MTT assay
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[PMID: 26804231] |
| WI-38 | IC50 |
1700 nM
Compound: SGI-1776
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Growth inhibition of human WI38 cells after 48 hrs by CCK8 assay
Growth inhibition of human WI38 cells after 48 hrs by CCK8 assay
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[PMID: 28523101] |
In Vitro
SGI-1776 free base (2.5, 5 μM) inhibits Pim-1 protein expression and Pim-1 kinase activity in SACC cells. SGI-1776 free base (2.5, 5 μM) causes cell cycle arrest and reduces cell proliferation in SACC-83 and SACC-LM cells[1].
SGI-1776 free base (5 μM) inhibits cell migration and invasiveness in both SACC-83 and SACC-LM cells. SGI-1776 free base (0, 2.5, or 5 μM) induces apoptosis via Caspase-3 activation[1].
SGI-1776 free base (5 µM) exerts inhibitory effects on both lipid accumulation and TG synthesis without affecting the number of adipocytes[2].
SGI-1776 free base (5 µM) inhibits adipogenesis particularly at an early phase of differentiation[2].
SGI-1776 free base (5 µM) decreases the expression of C/EBP-α and PPAR-γ and the phosphorylation levels of STAT-3 during adipocyte differentiation, and downregulates the protein and/or mRNA expression of FAS, leptin and RANTES during adipocyte differentiation[2].
SGI-1776 free base shows the significant activity against HO-8910 cells in a dose-dependent manner, with IC50 of (5.2±0.6) µM, and the inhibiting effect of SGI-1776 free base is sharply increased from 1.25 µM to 20 µM in vitro[3].
SGI-1776 free base inhibits the migration and invasion of HO-8910 cells in a dose-dependent manner, and the inhibiting migration and invasion rate of 5 µM[3].
SGI-1776 free base (2.5, 5 and 10 µM) decreases Pim-1 kinase activity of HO-8910 cells in a dose-dependent manner. Furthermore, the down-regulation of Pim-1 expression by SGI-1776 free base significantly inhibits cell viability, arrests cell in G1 phase, and inhibits the migration and invasion[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1025065-69-3
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Appearance Solid
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Molecular Weight 405.42
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Formel C20H22F3N5O
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Color White to yellow
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SMILES
CN1CCC(CC1)CNC2=NN3C(C=C2)=NC=C3C4=CC=CC(OC(F)(F)F)=C4
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (11)
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Journal Impact Factor
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Most Recent
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Science
2017 Dec 1;358(6367):eaan4368. PMID: 29191878 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Adv Sci (Weinh)
PIM1 Attenuates Innate Immunity to Foster Coronavirus Replication through Ubiquitin Ligase β-TrCP-Mediated IFNAR1 Degradation. [Abstract]2025 Jul 6:e03487. PMID: 40619619 -
Cell Death Dis
PIM1 mediates epithelial-mesenchymal transition by targeting Smads and c-Myc in the nucleus and potentiates clear-cell renal-cell carcinoma oncogenesis. [Abstract]2018 Feb 22;9(3):307. PMID: 29472550
SGI-1776 free base purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Feb 22;9(3):307. [Abstract]
PIM1 directly phosphorylated Smad2 and Smad3 and that inhibition of PIM1 kinase activity with SGI-1776 significantly reduces the protein levels of p-Smad2 and p-Smad3
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Phytomedicine
6''-O-acetylsaikosaponin D targets STAT3-mediated transcriptional remodeling to induce ferroptosis and apoptosis. [Abstract]2026 May 15:157:158301. PMID: 42166974 -
Cell Chem Biol
2024 Feb 15;31(2):326-337.e11. PMID: 38016478 -
J Med Chem
Discovery of a Dual Tubulin and Poly(ADP-Ribose) Polymerase-1 Inhibitor by Structure-Based Pharmacophore Modeling, Virtual Screening, Molecular Docking, and Biological Evaluation. [Abstract]2021 Nov 11;64(21):15702-15715. PMID: 34670362 -
Front Cell Infect Microbiol
ZIKV prM hijacks PIM1 kinase for phosphorylation to prevent ubiquitin-mediated degradation and facilitate viral replication. [Abstract]2024 Nov 29:14:1502770. PMID: 39679197 -
eNeuro
2019 Aug 22;6(4):ENEURO.0003-19.2019. PMID: 31387876 -
Anticancer Drugs
2024 Jan 1;35(1):46-54. PMID: 37449977 -
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 125 mg/mL (308.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.13 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.13 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
Kinase Assay[1]
SACC-83 free base and SACC-LM cells of 0 μM, 2.5 μM and 5 μM groups after SGI-1776 exposure are harvested. 6 samples of SACC cells are diluted in Kinase buffer and pipetted into the wells which is pre-coated with a substrate corresponding to recombinant p21waf1. It contains threonine residues that can be efficiently phosphorylated by Pim-1. After undergoing the procedure, measure absorbance in each well is quantitated by spectrophotometry at dual wavelengths of 450/540 nm. It reflects the relative amount of Pim-1 activity in the 6 groups of SACC cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay[3]
Cells are seeded in a 96-well plate at a density of 5 000 cells/well. After incubation for 24 h, different concentrations of SGI-1776 (0.625, 1.25, 2.5, 5, 10, 20, 40 µM) are added to each well and cultured for 48 h. The medium is removed and then incubated with 5 mg/L MTT for 4 h. Next, the supernatant is removed after centrifugation. Finally, 100 µL of DMSO is added and an absorbance at 570 nm wavelength (A570) is measured by enzyme-labeling instrument. Relative cell proliferation inhibition rate (IR)=(1-average A570 of the experimental group/average A570 of the control group)×100%.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration[4]
The conditions for animal room environment and photoperiod are 20-25°C, 40%-70% humidity, and 12 hours of light/12 hours of dark cycle. Each mouse is inoculated subcutaneously at the right flank with MV-4-11 tumor cells (5×106). The treatments start when the tumor size reach 80-150 mm3. Mice are randomized to treatment groups based on their tumor sizes; tumor size is measured in 2 dimensions using a caliper, and the volume is expressed in mm3 using the formula: V = 0.5 a × b2 where a and b are the long and short diameters of the tumor, respectively. Pretreatment randomization ensures that each group has approximately the same mean tumor size. Mice are treated with vehicle (5% dextrose), SGI-1776 or cytarabine (ara-C). SGI-1776 and ara-C are formulated in 5% dextrose. SGI-1776 is administered by oral gavage (PO) on a daily × 5/week or twice/week schedule; ara-C is administered by intraperitoneal injection 3 times/week for 3 consecutive weeks. Animals are euthanized when their measured tumor size is greater than 3000 mm3 or when they lose ≥ 20% initial body weight; if the body weight loss ≥ 15%, treatment is stopped at first until mice regain body weight. Mice are euthanized when body weight loss is still ≥ 20% even after stopping treatment. T/C value (in %) is an indication of antitumor efficacy, where T and C are the mean tumor volume of the treated and control groups, respectively, on a given day. The differences between the mean tumor sizes for comparing groups is analyzed using the ANOVA test, where P ≤ 0.05 is considered to be statistically significant.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (281 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Hou X, et al. Biochemical changes of salivary gland adenoid cystic carcinoma cells induced by SGI-1776. Exp Cell Res. 2017 Mar 15;352(2):403-411. [Content Brief]
[2]. Park YK, et al. The novel anti-adipogenic effect and mechanisms of action of SGI-1776, a Pim-specific inhibitor, in 3T3-L1 adipocytes. Int J Mol Med. 2016 Jan;37(1):157-64 [Content Brief]
[3]. Xie J, et al. SGI-1776, an imidazo pyridazine compound, inhibits the proliferation of ovarian cancer cells by inactivating Pim-1. Zhong Nan Da Xue Xue Bao Yi Xue Ban. 2014 Jul;39(7):649-57 [Content Brief]
[4]. Chen LS, et al. Mechanisms of cytotoxicity to Pim kinase inhibitor, SGI-1776, in acute myeloid leukemia. Blood, 2011, 118(3), 693-702. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4666 mL | 12.3329 mL | 24.6658 mL | 61.6644 mL |
| 5 mM | 0.4933 mL | 2.4666 mL | 4.9332 mL | 12.3329 mL | |
| 10 mM | 0.2467 mL | 1.2333 mL | 2.4666 mL | 6.1664 mL | |
| 15 mM | 0.1644 mL | 0.8222 mL | 1.6444 mL | 4.1110 mL | |
| 20 mM | 0.1233 mL | 0.6166 mL | 1.2333 mL | 3.0832 mL | |
| 25 mM | 0.0987 mL | 0.4933 mL | 0.9866 mL | 2.4666 mL | |
| 30 mM | 0.0822 mL | 0.4111 mL | 0.8222 mL | 2.0555 mL | |
| 40 mM | 0.0617 mL | 0.3083 mL | 0.6166 mL | 1.5416 mL | |
| 50 mM | 0.0493 mL | 0.2467 mL | 0.4933 mL | 1.2333 mL | |
| 60 mM | 0.0411 mL | 0.2055 mL | 0.4111 mL | 1.0277 mL | |
| 80 mM | 0.0308 mL | 0.1542 mL | 0.3083 mL | 0.7708 mL | |
| 100 mM | 0.0247 mL | 0.1233 mL | 0.2467 mL | 0.6166 mL |
SGI-1776 free base Related Classifications
HY-13287 Related Classifications
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