| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| References | |
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| Additional Infomation |
Darizmetinib is a small molecule drug. Its International Nonproprietary Name (INN) prefix "-tinib" indicates that darizmetinib is a tyrosine kinase inhibitor. The monoisotopic molecular weight of darizmetinib is 457.1 Da. Darizmetinib is an orally bioavailable mitogen-activated protein kinase (MAP) kinase 4 (MKK4; MAP2K4) inhibitor with potential hepatoprotective, proliferative, and liver regeneration effects. After oral administration, darizmetinib selectively targets, binds to, and inhibits MKK4 activity in hepatocytes. This allows the MKK7 and mitogen-activated protein kinase 8 (MAPK8; MAP2K1) proliferation-enhancing pathways to be activated, which in turn activate the transcription factor ATF2 and the ETS domain protein ELK1. This promotes hepatocyte proliferation, increases hepatocyte survival, and promotes liver regeneration after hepatectomy. This may help prevent liver failure, restore liver quality, and protect hepatocytes from death. MKK4 is a MAP2K and part of the stress-activated protein kinase (SAPK)/mitogen-activated protein kinase (MAPK) signaling pathway, playing a crucial role in inhibiting cell proliferation and regulating hepatocyte regeneration. Inhibiting MKK4 can enhance the regenerative capacity of hepatocytes.
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| Molecular Formula |
C21H17F2N5O3S
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|---|---|
| Molecular Weight |
457.453189611435
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| Exact Mass |
457.102
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| CAS # |
2369583-33-3
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| PubChem CID |
139369660
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| Appearance |
White to off-white solid powder
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| LogP |
3.1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
32
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| Complexity |
761
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(CCC)(NC1C(=CC=C(C(C2=C3C=C(C=NC3=NN2)C2C=CN=CC=2)=O)C=1F)F)(=O)=O
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| InChi Key |
WBNMARNYIFMNEP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H17F2N5O3S/c1-2-9-32(30,31)28-19-16(22)4-3-14(17(19)23)20(29)18-15-10-13(11-25-21(15)27-26-18)12-5-7-24-8-6-12/h3-8,10-11,28H,2,9H2,1H3,(H,25,26,27)
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| Chemical Name |
N-[2,6-difluoro-3-(5-pyridin-4-yl-2H-pyrazolo[3,4-b]pyridine-3-carbonyl)phenyl]propane-1-sulfonamide
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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 | 2.1860 mL | 10.9302 mL | 21.8603 mL | |
| 5 mM | 0.4372 mL | 2.1860 mL | 4.3721 mL | |
| 10 mM | 0.2186 mL | 1.0930 mL | 2.1860 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.
Products are for research use only; We do not sell to patients
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