| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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1G244 is a novel and potent DPP8/9 inhibitor (IC50s = 12 nM and 84 nM, respectively) with anticancer activity. It does not inhibit DPPIV and DPPII.
| ln Vitro |
In five different multiple myeloma cell lines, 1G244 (0-100 μM; 72 hours; Delta47, U266, KMS-5, RPMI8226, or MM.1 S cells) formulations were found to lower viable cell counts in a desirable way [1]. 50 μM; 0-48 hours; MM.1 S cells) stimulates cells due to the detection of indoor forms of PARP and caspase-3 [1].
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| ln Vivo |
In a mouse xenograft tumor model, 1G244 (30 mg/kg; subcutaneous injection; once weekly; for 3 weeks; NOG female mice) effectively reduced the subcutaneous growth of MM.1S cells [1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: Delta47, U266, KMS-5, RPMI8226 or MM.1 S Cell Tested Concentrations: 0 μM, 1 μM, 5 μM, 10 μM, 50 μM or 100 μM Incubation Duration: 72 hrs (hours) Experimental Results: There was a dose-dependent decrease in viable cell numbers in five multiple myeloma cell lines. Western Blot Analysis [1] Cell Types: MM.1 S cell Tested Concentrations: 50 μM Incubation Duration: 0 hrs (hours), 3 hrs (hours), 6 hrs (hours), 12 hrs (hours), 24 hrs (hours), 48 hrs (hours) Experimental Results: caspase-3 and PARP proteins were diminished. |
| Animal Protocol |
Animal/Disease Models: NOD/Shi -scid IL-2Rγnull (NOG) female mice (6-7 weeks; 19-21 g) were injected with MM.1 S cells [1]
Doses: 30 mg/kg Route of Administration: subcutaneous injection; Once a week; last for 3 weeks. Experimental Results: Dramatically inhibited the subcutaneousgrowth of MM.1 S cells in mouse xenograft model. |
| References |
| Molecular Formula |
C29H30F2N4O2
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|---|---|
| Molecular Weight |
504.570913791656
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| Exact Mass |
504.233
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| CAS # |
847928-32-9
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| PubChem CID |
56658139
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
2.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
37
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| Complexity |
740
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C(C1C=CC(F)=CC=1)(C1C=CC(F)=CC=1)N1CCN(C(=O)C[C@H](N)C(N2CC3C=CC=CC=3C2)=O)CC1
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| InChi Key |
ZKIQFLSGMMYCGS-SANMLTNESA-N
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| InChi Code |
InChI=1S/C29H30F2N4O2/c30-24-9-5-20(6-10-24)28(21-7-11-25(31)12-8-21)34-15-13-33(14-16-34)27(36)17-26(32)29(37)35-18-22-3-1-2-4-23(22)19-35/h1-12,26,28H,13-19,32H2/t26-/m0/s1
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| Chemical Name |
(S)-2-Amino-4-{4-[bis-(4-fluorophenyl)-methyl]piperazin-1-yl}-1-(1,3-dihydro-isoindol-2-yl)-butane-1,4-dione
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| Synonyms |
1G-244 1G 2441G244
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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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~250 mg/mL (~495.47 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.12 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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL 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: ≥ 2.08 mg/mL (4.12 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 20.8 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 | 1.9819 mL | 9.9094 mL | 19.8189 mL | |
| 5 mM | 0.3964 mL | 1.9819 mL | 3.9638 mL | |
| 10 mM | 0.1982 mL | 0.9909 mL | 1.9819 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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