| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
Syk-IN-11 selectively targets Syk with a binding Kd of 0.64 nM, demonstrating 100-fold binding selectivity over ZAP70 (Kd = 65 nM). Its chemical structure comprises a 7-aminoindole moiety coupled to a substituted 1,2,4-triazine core.
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|---|---|
| ln Vitro |
In vitro, Syk-IN-11 shows potent enzymatic inhibition with a cellular IC50 of 99 nM in BCR signaling assays and an ex vivo blood IC50 of 189 nM for FcγR-mediated SLP76 phosphorylation. It is a next-generation Syk inhibitor with enhanced selectivity.
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| ln Vivo |
Syk-IN-11 has demonstrated in vivo efficacy in rat models of collagen-induced arthritis (CIA) at doses of 3-30 mg/kg. It is orally bioavailable with good pharmacokinetic properties in rodents and dogs.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays typically involve evaluating Syk-IN-11's inhibitory activity against purified Syk kinase using ATP-competitive binding assays. IC50 or Kd values are determined by measuring residual kinase activity after incubation with varying concentrations of the compound.
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| Cell Assay |
For in vitro cell-based assays, Syk-IN-11 is dissolved in DMSO and applied to cultured immune cells such as B cells or mast cells at concentrations ranging from 10 nM to 10 µM. Effects on BCR signaling, degranulation, or cytokine production are assessed after 1-24 hours of treatment.
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| Animal Protocol |
In vivo animal studies commonly use rat CIA models. Syk-IN-11 is administered orally at doses of 3-30 mg/kg. Efficacy is evaluated by measuring clinical arthritis scores, paw swelling, and histopathological examination of joint tissues.
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| ADME/Pharmacokinetics |
Syk-IN-11 has favorable oral bioavailability in rodents and dogs. It is soluble in DMSO and is typically stored as a powder at -20°C for long-term stability.
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| Toxicity/Toxicokinetics |
In preclinical studies, Syk-IN-11 has demonstrated a favorable safety profile with minimal off-target kinase activity. No significant toxicity has been reported at therapeutic doses in animal models.
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| References | |
| Additional Infomation |
Syk-IN-11 is a well-characterized tool compound for preclinical autoimmune and oncology research. It is used to study Syk pathway inhibition in B-cell and myeloid signaling contexts. Its discovery and profiling have been published in the Journal of Medicinal Chemistry.
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| Molecular Formula |
C18H22N8O
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|---|---|
| Molecular Weight |
366.420281887054
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| Exact Mass |
366.191
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| CAS # |
1491150-77-6
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| PubChem CID |
72202597
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
1.7
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
520
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| Defined Atom Stereocenter Count |
2
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| SMILES |
O=C(C1=C(NC2C=CC=C3C=CNC=23)N=C(N=N1)N[C@@H]1CCCC[C@@H]1N)N
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| InChi Key |
FPQNRXITKTZFMF-NWDGAFQWSA-N
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| InChi Code |
InChI=1S/C18H22N8O/c19-11-5-1-2-6-12(11)23-18-24-17(15(16(20)27)25-26-18)22-13-7-3-4-10-8-9-21-14(10)13/h3-4,7-9,11-12,21H,1-2,5-6,19H2,(H2,20,27)(H2,22,23,24,26)/t11-,12+/m0/s1
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| Chemical Name |
3-[[(1R,2S)-2-aminocyclohexyl]amino]-5-(1H-indol-7-ylamino)-1,2,4-triazine-6-carboxamide
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| Synonyms |
SykIN11; Syk IN 11; Syk-IN-11
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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) |
DMSO : ~100 mg/mL (~272.91 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (13.65 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 50.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7291 mL | 13.6455 mL | 27.2911 mL | |
| 5 mM | 0.5458 mL | 2.7291 mL | 5.4582 mL | |
| 10 mM | 0.2729 mL | 1.3646 mL | 2.7291 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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