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JAK3 Inhibitor VI is a novel and potent inhibitor of Janus kinase 3 (JAK3) with anti-AML (acute myeloid leukemia) activity. Exhibits IC50s of ∼40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively.
| ln Vitro |
JI6 (3-1000 nM; 1-4 days) has an IC50 value of around 25 nM and reduces MV4-11 cell viability in a suspended dosage manner [1]. JI6 (1-2000 nM; 48 h) is generally ineffective against parental HCD-57 or cells expressing JAK2V617F, but it effectively suspends the viability of HCD-57 cells expressing FLT3-ITD, FLT3-D835Y, and FLT3-D835H, with an IC50 value of ∼40 nM. Not at all[1]. HCD-57 cells and cell cycle marketing are used to induce JI6 (100-500 nM; 24 h) JI6 (50-500 nM; 3 h) GFP FLT3-ITD and FLT3-D835Y[1].
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| ln Vivo |
JI6 (15 mg/kg; ip daily for 3 weeks) suppresses the proliferation and prolongs the duration of mold in HCD-57 expressing FLT3-D835Y within immunodeficient microarrays [1]. JI6 (25 mg/kg; po daily for 3 weeks) JI6 (100 mg/kg; a single ip) effectively suppresses FLT3 phosphorylation and downstream signaling in clocks expressing FLT3-D835Y [ ) Inhibition of FLT3- Ischemic potential phenotype of ITD knock-in mice [1].
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| Cell Assay |
Cell viability assay[1] cells Lines: MV4-11, HL60, Karpas 299 and Jurkat cells
Tested Concentrations: 3-1000 nM Incubation Duration: 48 hrs (hours) Experimental Results: Inhibited phosphorylation of FLT3 and ERK and Akt in 57 cells [1]. MV4-11 cells at concentrations up to JI6 at 1 μM had no effect on the remaining three cells. Apoptosis analysis[1] Cell Types: FLT3-ITD and FLT3-D835Y transformed HCD-57 cells Tested Concentrations: 100, 500 nM Incubation Duration: 24 hrs (hours) Experimental Results: Apoptosis and increased percentage of necrotic cells, with no effect on apoptosis of parental HCD-57 cells. Cell cycle analysis [1] Cell Types: FLT3-ITD and FLT3-D835Y Transformed HCD-57 cells Tested Concentrations: 100, 500 nM Incubation Duration: 24 hrs (hours) Experimental Results: G2 and S phase cells diminished Dramatically, G1 phase cells increased FLT3-ITD and D835Y cells. Cell viability assay [1] Cell Types: FLT3-ITD and FLT3-D835Y transformed HCD-57 cells Tested Concentrations: 50, 100, 500 nM Incubation Duration: 3 hrs (hours) Experimental Results: Phosphorylation of FLT3, ERK1, ERK2, and Akt was inhi |
| Animal Protocol |
Animal/Disease Models: NSG mice (10-12 weeks old, male) were implanted with FLT3-D835Y transformed HCD-57 cells [1]
Doses: 15 mg/kg Route of Administration: daily intraperitoneal (ip) injection for 3 weeks Experimental Results: spleen diminished size and extended the survival time of these mice. |
| References | |
| Additional Infomation |
5-(3-pyridinyl)-3-(1H-pyrrol-2-ylmethylidene)-1H-indol-2-one is a member of indoles.
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| Molecular Formula |
C19H17N3O4S
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|---|---|
| Molecular Weight |
383.42
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| Exact Mass |
383.094
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| CAS # |
856436-16-3
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| PubChem CID |
9947841
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
4.292
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
22
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| Complexity |
461
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CS(=O)(=O)O.C1=CC(=CN=C1)C2=CC3=C(C=C2)NC(=O)C3=CC4=CC=CN4
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| InChi Key |
IQNTXIMXKCURDC-YBEGLDIGSA-N
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| InChi Code |
InChI=1S/C18H13N3O/c22-18-16(10-14-4-2-8-20-14)15-9-12(5-6-17(15)21-18)13-3-1-7-19-11-13/h1-11,20H,(H,21,22)/b16-10-
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| Chemical Name |
(3Z)-5-pyridin-3-yl-3-(1H-pyrrol-2-ylmethylidene)-1H-indol-2-one
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| Synonyms |
JAK 3 Inhibitor VI JAK-3 Inhibitor VI JAK3 Inhibitor VI
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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 | 2.6081 mL | 13.0405 mL | 26.0811 mL | |
| 5 mM | 0.5216 mL | 2.6081 mL | 5.2162 mL | |
| 10 mM | 0.2608 mL | 1.3041 mL | 2.6081 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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