| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 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 an integrin-targeted PI3 kinase inhibitor.
pan-PI3K/mTOR Inhibitor SF1126 is a water soluble, small-molecule prodrug containing the pan-PI3K/mTOR inhibitor LY294002/SF1101 conjugated to the RGD-containing tetra-peptide SF1174 with potential antineoplastic and antiangiogenic activities. The targeting peptide SF1174 moiety of pan-PI3K/mTOR inhibitor SF1126 selectively binds to cell surface integrins and, upon cell entry, the agent is hydrolyzed to the active drug SF1101; SF1101 selectively inhibits all isoforms of phosphoinositide-3-kinase (PI3K) and other members of the PI3K superfamily, such as the mammalian target of rapamycin (mTOR) and DNA-PK. By inhibiting the PI3K signaling pathway, this agent may inhibit tumor cell and tumor endothelial cell proliferation and survival. Drug Indication For the treatment of various forms of cancer. Mechanism of Action SF1126 is a small molecule conjugate containing a pan-PI3K inhibitor that selectively inhibits all PI3K class IA isoforms and other key members of the PI3K superfamily, including DNA-PK and mTOR. A major factor in tumor resistance to approved chemotherapy agents is thought to be the activation of the PI3K/PTEN pathway. As a result, it is thought that inhibiting this pathway, via SF1126, could cause the resetting of sensitivity to approved agents and exhibit synergistic anticancer effects. Pharmacodynamics SF1126 is a covalent conjugate of LY294002 that contains a peptide-based targeting group to help increase the localization of the drug in the neovascular component supporting tumor growth. SF1126 is a highly water soluble solid which aids its administration via i.v. or s.c. injections. In vivo it converts spontaneously at physiological pH to LY294002 in a way that is well tolerated in mice, rats, and dogs. SF1126 has been evaluated in numerous animal tumor models showing good tumor inhibition or tumor regression. |
| Molecular Formula |
C39H48N8O14
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|---|---|
| Molecular Weight |
852.8436
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| Exact Mass |
912.35
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| CAS # |
936487-67-1
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| PubChem CID |
66577114
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| Appearance |
White to off-white solid powder
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| LogP |
0.074
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
15
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| Rotatable Bond Count |
22
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| Heavy Atom Count |
61
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| Complexity |
1650
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| Defined Atom Stereocenter Count |
3
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| 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
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| InChi Key |
SVNJBEMPMKWDCO-KCHLEUMXSA-N
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| 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
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| 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
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| HS Tariff Code |
2934.99.9001
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| 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)
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| 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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