| Size | Price | |
|---|---|---|
| 1mg | ||
| 5mg | ||
| Other Sizes |
| ln Vitro |
Hep3B, HepG2, SK-Hep1, and Huh7 cell proliferation is inhibited by SF1126 (0–6 µM; 48 hours), with IC50 values of 5.05, 6.89, 3.14, and 2.14 µM, respectively [1]. Hep 3B, Hep G2, SK-Hep1, and Huh7 cell cycle arrest are caused by SF1126 (1-10 µM; 24 hr); this results in a proportionate rise in G0-G1 and a decrease in S-phase cells [1]. Combination treatment with SF1126 and sorafenib (0.5-2.5 µM; 30 minutes ago) has been demonstrated to block multiple key enzymes in the Ras/Raf/MAPK and PI3K/AKT/mTOR pathways[1].
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|---|---|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: Hep3B, HepG2, SK-Hep1 and Huh7 Cell Tested Concentrations: 0 µM; 1 µM; 2 µM; 3 µM; 4 µM; 5 µM; 6 µM Incubation Duration: 48 hrs (hours) Experimental Results: Enhanced inhibition of HCC proliferation. Cell cycle analysis[1] Cell Types: Hep3B, HepG2, SK-Hep1 and Huh7 Cell Tested Concentrations: 1 µM; 5µM; 10 µM Incubation Duration: 24 hrs (hours) Experimental Results: Induction of cell cycle arrest. Western Blot Analysis[1] Cell Types: Hep3B, HepG2, SK-Hep1 and Huh7 Cell Tested Concentrations: 0.5 µM and 2.5 µM Incubation Duration: 30 minutes ago Experimental Results: Phosphorylation of AKT, p70S6K, 4EBP1 and ERK was inhibited in all cells Cell lines and sorafenib. |
| References | |
| Additional Infomation |
SF1126 is a PI3 kinase inhibitor targeting integrins. The pan-PI3K/mTOR inhibitor SF1126 is a water-soluble small molecule prodrug conjugated to the pan-PI3K/mTOR inhibitor LY294002/SF1101 and the tetrapeptide SF1174 containing the RGD sequence, exhibiting potential antitumor and anti-angiogenic activity. The targeting peptide SF1174 of the pan-PI3K/mTOR inhibitor SF1126 selectively binds to cell surface integrins. Upon entry into the cell, the drug is hydrolyzed to the active drug SF1101. SF1101 selectively inhibits all phosphatidylinositol-3-kinase (PI3K) isoforms and other members of the PI3K superfamily, such as mammalian target of rapamycin (mTOR) and DNA-PK. By inhibiting the PI3K signaling pathway, this drug may inhibit the proliferation and survival of tumor cells and tumor endothelial cells. Drug Indications: For the treatment of various cancers. Mechanism of Action SF1126 is a small molecule conjugate containing a pan-PI3K inhibitor that selectively inhibits all PI3K class IA subtypes and other key members of the PI3K superfamily, including DNA-PK and mTOR. A major factor contributing to tumor resistance to approved chemotherapeutic agents is believed to be the activation of the PI3K/PTEN pathway. Therefore, it is thought that inhibiting this pathway by SF1126 could reset sensitivity to approved drugs and exhibit synergistic anticancer effects. Pharmacodynamics SF1126 is a covalent conjugate of LY294002 containing a peptide-based targeting group, which helps improve the drug's localization to the angiogenic components that support tumor growth. SF1126 is a highly water-soluble solid, facilitating intravenous or subcutaneous administration. In vivo, it spontaneously converts to LY294002 under physiological pH conditions and is well-tolerated in mice, rats, and dogs. SF1126 has been evaluated in various animal tumor models, and the results show that it has good tumor inhibition or tumor regression effects.
|
| Molecular Formula |
C39H48N8O14
|
|---|---|
| Molecular Weight |
852.8436
|
| Exact Mass |
912.35
|
| CAS # |
936487-67-1
|
| PubChem CID |
66577114
|
| Appearance |
White to off-white solid powder
|
| LogP |
0.074
|
| Hydrogen Bond Donor Count |
8
|
| Hydrogen Bond Acceptor Count |
15
|
| Rotatable Bond Count |
22
|
| Heavy Atom Count |
61
|
| Complexity |
1650
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
C1COCC[N+]1(COC(=O)CCC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)[O-])C2=CC(=O)C3=C(O2)C(=CC=C3)C4=CC=CC=C4
|
| InChi Key |
SVNJBEMPMKWDCO-KCHLEUMXSA-N
|
| InChi Code |
InChI=1S/C39H48N8O14/c40-39(41)42-13-5-10-26(36(55)43-20-31(51)45-27(18-33(52)53)37(56)46-28(21-48)38(57)58)44-30(50)11-12-34(54)60-22-47(14-16-59-17-15-47)32-19-29(49)25-9-4-8-24(35(25)61-32)23-6-2-1-3-7-23/h1-4,6-9,19,26-28,48H,5,10-18,20-22H2,(H9-,40,41,42,43,44,45,46,50,51,52,53,55,56,57,58)/t26-,27-,28-/m0/s1
|
| Chemical Name |
(2S)-2-[[(2S)-3-carboxy-2-[[2-[[(2S)-5-(diaminomethylideneamino)-2-[[4-oxo-4-[[4-(4-oxo-8-phenylchromen-2-yl)morpholin-4-ium-4-yl]methoxy]butanoyl]amino]pentanoyl]amino]acetyl]amino]propanoyl]amino]-3-hydroxypropanoate
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1726 mL | 5.8628 mL | 11.7255 mL | |
| 5 mM | 0.2345 mL | 1.1726 mL | 2.3451 mL | |
| 10 mM | 0.1173 mL | 0.5863 mL | 1.1726 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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