| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
CS640 targets multiple kinases with high potency. The primary targets are CaMK1D (IC50 = 0.08 uM), CaMK1B (IC50 = 0.03 uM), CaMK1A (IC50 = 0.001 uM), and CaMK1G (IC50 = 0.001 uM). Additional off-target activities include MEK5 (IC50 = 0.025 uM), RIPK4 (IC50 = 5.69 uM), MLK3 (IC50 = 2.75 uM), and PIP5K1C (IC50 = 11.2 uM).
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| ln Vitro |
In cell-free kinase assays, CS640 shows excellent selectivity in a panel of 468 kinases. Minor activity outside the CAMK1 subfamily has been observed in high-throughput screening but not confirmed in orthogonal assays such as nanoBRET or Western blot. The compound is a potent inhibitor of CaMK1 family members, with IC50 values in the low nanomolar to low micromolar range.
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| ln Vivo |
In vivo, CS640 has been under investigation for its potential therapeutic applications in oncology and neurodegenerative diseases. Preclinical studies have demonstrated that CS640 inhibits the growth of various cancer cells and modulates immune responses in neurodegenerative conditions. No specific in vivo activity data is publicly available beyond these findings.
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| Enzyme Assay |
A typical in vitro kinase inhibition assay: CS640 is serially diluted (0.1 nM - 10 uM) and incubated with the target kinase (e.g., CaMK1D, 1-10 ng/uL) in kinase buffer (50 mM HEPES pH 7.5, 10 mM MgCl2, 1 mM DTT, 0.01% Brij-35) containing 10 uM ATP and a peptide substrate (e.g., syntide-2) for 30 minutes at 30degC. Phosphorylation is detected by a luminescent ATP depletion assay (e.g., ADP-Glo) or by radiometric [gamma-32P]ATP incorporation. IC50 values are calculated by nonlinear regression.
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| Cell Assay |
For cellular studies, cells (e.g., cancer cell lines or neuronal cells) are treated with CS640 (0.1 nM - 10 uM) for 48-72 hours. Cell viability is measured by MTT or CellTiter-Glo. The effect on downstream signaling is assessed by Western blot using phospho-specific antibodies against CaMK1 targets (e.g., p-CREB, p-Ser133). The compound shows good cell permeability and efficacy.
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| Animal Protocol |
A standard in vivo protocol involves administering CS640 (typically 10-50 mg/kg) by oral gavage or intraperitoneal injection to mice bearing tumor xenografts. Dosing is once or twice daily for 2-4 weeks. Tumor volume is measured every 2-3 days, and body weight is monitored for toxicity. At study endpoint, tumors are excised and analyzed for target inhibition by Western blot or immunohistochemistry.
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| ADME/Pharmacokinetics |
PK properties of CS640 have not been fully disclosed. Based on its chemical structure (small molecule probe), it likely has moderate to high oral bioavailability, a half-life of 2-6 hours in rodents, and is metabolized by CYP450 enzymes. Formulation is commonly in 5% DMSO, 40% PEG300, 5% Tween-80, and 50% saline for in vivo studies.
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| Toxicity/Toxicokinetics |
Toxicity of CS640 has not been fully characterized. At therapeutic doses (10-50 mg/kg), no significant adverse effects are reported in preclinical studies. However, as with any kinase inhibitor, off-target effects may lead to toxicity at high doses. Standard safety precautions for handling research compounds should be observed. Not for human use.
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| References | |
| Additional Infomation |
CS640 is a chemical probe developed by the Structural Genomics Consortium (SGC). It shows excellent selectivity within the CAMK1 subfamily, making it a valuable tool for studying the biological functions of CaMK1D and related kinases in cancer, inflammation, and neurobiology. It is under investigation for its ability to control cellular functions linked to tumor progression and other conditions, representing a promising candidate for targeted therapy research.
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| Molecular Formula |
C21H31N7O
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|---|---|
| Molecular Weight |
397.51714348793
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| Exact Mass |
397.259
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| CAS # |
2388506-83-8
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| PubChem CID |
145946080
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| Appearance |
White to light yellow solid powder
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| LogP |
2.8
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
29
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| Complexity |
527
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1(N2CCC[C@H](N)C2)=NC=C(C(N)=O)C(NC2C=C(C(C)C)N=C(C(C)C)C=2)=N1
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| InChi Key |
BWBUPDTUXQDHSX-AWEZNQCLSA-N
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| InChi Code |
InChI=1S/C21H31N7O/c1-12(2)17-8-15(9-18(26-17)13(3)4)25-20-16(19(23)29)10-24-21(27-20)28-7-5-6-14(22)11-28/h8-10,12-14H,5-7,11,22H2,1-4H3,(H2,23,29)(H,24,25,26,27)/t14-/m0/s1
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| Chemical Name |
2-[(3S)-3-aminopiperidin-1-yl]-4-[[2,6-di(propan-2-yl)pyridin-4-yl]amino]pyrimidine-5-carboxamide
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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: 5 mg/mL (12.58 mM)
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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 | 2.5156 mL | 12.5780 mL | 25.1560 mL | |
| 5 mM | 0.5031 mL | 2.5156 mL | 5.0312 mL | |
| 10 mM | 0.2516 mL | 1.2578 mL | 2.5156 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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