| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
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SG3199 is a PBD dimer which binds in the minor groove of DNA, and forms covalent DNA interstrand cross-links in naked linear plasmid DNA. SG3199 is potently cytotoxic against a panel of human solid tumour and haematological cancer cell lines.
| ln Vitro |
SG3199 exhibits strong cytotoxicity, with an average GI50 of 151.5 pM, against a range of solid tumors and blood DNA lines in humans. Cells lacking homologous recombination repair (HRR) or the DNA repair protein ERCC1 are weighted higher at SG3199, which is only multidrug-general. Cross-linking in dosage is seen in cells, and SG3199 produces DNA interstrand cross-linking mechanisms in bare linear DNA [1].
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| ln Vivo |
At doses of 0.8, 5, and 50 ng/mL, the antibiotic binding of [3H]-SG3199 with adjuvant (Sprague Dawley), monkey, and human antibiotics was measured. All species have comparable rates of antibiotic binding: 97% in humans, 90% in cynomolgus monkeys, and 95% in other species [1]. After receiving intravenous infusion at 0.1 μg/kg, 0.5 μg/kg, and 1 μg/kg, SG3199 demonstrated extremely quick clearance in FX. T1/2 ranged from 8 to 42 minutes, and fast clearance was observed in the 0.5 μg/kg and 1 μg/kg dosage groups between 1000 and 1500 mL/h/kg [1].
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| References |
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| Molecular Formula |
C33H36N4O6
|
|---|---|
| Molecular Weight |
584.662148475647
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| Exact Mass |
584.263
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| CAS # |
1595275-71-0
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| Related CAS # |
1595275-71-0
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| PubChem CID |
90132565
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| Appearance |
White to off-white solid powder
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| LogP |
2.8
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
43
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| Complexity |
1080
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| Defined Atom Stereocenter Count |
2
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| SMILES |
O(CCCCCOC1C(=CC2=C(C=1)N=C[C@@H]1CC(C)=CN1C2=O)OC)C1C(=CC2=C(C=1)N=C[C@@H]1CC(C)=CN1C2=O)OC
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| InChi Key |
YMTZZJOPSATRTO-GOTSBHOMSA-N
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| InChi Code |
InChI=1S/C33H36N4O6/c1-20-10-22-16-34-26-14-30(28(40-3)12-24(26)32(38)36(22)18-20)42-8-6-5-7-9-43-31-15-27-25(13-29(31)41-4)33(39)37-19-21(2)11-23(37)17-35-27/h12-19,22-23H,5-11H2,1-4H3/t22-,23-/m0/s1 SMILES
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| Chemical Name |
(11aS,11a'S)-8,8'-(Pentane-1,5-diylbis(oxy))bis(7-methoxy-2-methyl-1,11a-dihydro-5H-benzo[e]pyrrolo[1,2-a][1,4]diazepin-5-one)
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| Synonyms |
SG-3199 SG 3199 SG3199
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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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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) |
DMSO : ~130 mg/mL (~222.35 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3.25 mg/mL (5.56 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 32.5 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 3.25 mg/mL (5.56 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 32.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7104 mL | 8.5520 mL | 17.1040 mL | |
| 5 mM | 0.3421 mL | 1.7104 mL | 3.4208 mL | |
| 10 mM | 0.1710 mL | 0.8552 mL | 1.7104 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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