| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
Inducing apoptosis and inhibiting cell proliferation, PD184161 (1–20 μM) exhibits concentration- and time-dependent effects [1]. A one-hour dose of 0.1 and 1.0 μM PD184161,2 inhibits phosphorylation of ERK1,2 [1]. PD184161 (5 μM; 30 min) protects against the toxic effects of bicuculline [3].
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| ln Vivo |
After oral administration, PD184161 decreases P-ERK levels in tumor xenografts in 3–12 hours [1]. PD184161, administered orally twice daily for 38 days at a dose of 300 mg/kg, dramatically slowed the growth and implantation of tumors [1]. A single injection of PD184161, at a dose of 30 mg/kg, induces depressive-like symptoms [2]. After a stroke, PD184161, administered intravenously at a dose of 500 μg/kg, stops the progression of neurological impairments and brain damage [3].
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: HCC cell lines (HepG2, Hep3B, PLC and SKHep) Tested Concentrations: 1-20 μM Incubation Duration: 24, 48 or 72 hrs (hours) Experimental Results: Cell proliferation was inhibited. Apoptosis analysis[1] Cell Types: HCC cell lines (HepG2, Hep3B, PLC and SKHep) Tested Concentrations: 1-20 μM Incubation Duration: 48 hrs (hours) Experimental Results: Induction of apoptosis. Western Blot Analysis[1] Cell Types: HCC cell lines (HepG2, Hep3B, PLC and SKHep) Tested Concentrations: 0.1 and 1.0 μM Incubation Duration: 1 hour Experimental Results: ERK1,2 phosphorylation is inhibited. Cell viability assay[3] Cell Types: Primary Mouse Neurons Tested Concentrations: 5 μM Incubation Duration: 30 min Experimental Results: Protection against toxic effects of bicuculline. |
| Animal Protocol |
Animal/Disease Models: Hep3B tumor xenograft BALB/c athymic nude mice [1]
Doses: 300 mg/kg Route of Administration: Orogastric gavage, twice a day for 38 days Experimental Results: diminished early tumor growth. Animal/Disease Models: Male, 6weeks old C57Bl/6 mice [2] Doses: 500 μg/kg Route of Administration: intravenous (iv) (iv)injection 30 minutes before MCAO or PTZ administration Experimental Results: Prevent the progression of neurological deficits and brain damage after stroke. Animal/Disease Models: C57Bl/6 mice [3] Doses: 30 mg/kg Route of Administration: intraperitoneal (ip) injection, single injection Experimental Results:depressive-like behavior. |
| References |
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| Molecular Formula |
C17H13BRCLF2IN2O2
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|---|---|
| Molecular Weight |
557.55
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| Exact Mass |
555.886
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| CAS # |
212631-67-9
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| PubChem CID |
9937619
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| Appearance |
Off-white to gray solid powder
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| Density |
1.9±0.1 g/cm3
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| Index of Refraction |
1.670
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| LogP |
9.28
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
26
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| Complexity |
505
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
VJNZMSLGVUSPCF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H13BrClF2IN2O2/c18-11-6-10(17(25)24-26-7-8-1-2-8)16(15(21)14(11)20)23-13-4-3-9(22)5-12(13)19/h3-6,8,23H,1-2,7H2,(H,24,25)
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| Chemical Name |
5-bromo-2-(2-chloro-4-iodoanilino)-N-(cyclopropylmethoxy)-3,4-difluorobenzamide
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| Synonyms |
PD184161; PD 184161; PD184161
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~100 mg/mL (~179.35 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (4.48 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: ≥ 2.5 mg/mL (4.48 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 25.0 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 | 1.7936 mL | 8.9678 mL | 17.9356 mL | |
| 5 mM | 0.3587 mL | 1.7936 mL | 3.5871 mL | |
| 10 mM | 0.1794 mL | 0.8968 mL | 1.7936 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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