| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
Haspin-IN-3 targets Haspin kinase (also known as GSG2), a serine/threonine protein kinase that plays a critical role in mitosis. Haspin phosphorylates histone H3 at threonine 3 (H3T3), which is essential for proper chromosome alignment, kinetochore function, and mitotic progression. By inhibiting Haspin with an IC₅₀ of 14 nM, Haspin-IN-3 disrupts H3T3 phosphorylation, leading to chromosome misalignment, mitotic delay, and apoptosis. This mechanism makes Haspin a potential therapeutic target in cancer, and Haspin-IN-3 is used as a research tool to study Haspin biology.
|
|---|---|
| ln Vitro |
In vitro, Haspin-IN-3 demonstrates potent Haspin inhibition with an IC₅₀ of 14 nM. The compound has anticancer effects. By inhibiting Haspin kinase, Haspin-IN-3 reduces histone H3 phosphorylation at threonine 3 (H3T3), leading to chromosome misalignment and mitotic arrest. This results in the inhibition of cancer cell proliferation and induction of apoptosis. The compound is used as a research tool to study the role of Haspin in mitosis and cancer. Further in vitro studies would be needed to fully characterize its activity and selectivity.
|
| ln Vivo |
In vivo, Haspin-IN-3 has potential for anticancer therapy. As a potent Haspin inhibitor, the compound may inhibit tumor growth through disruption of mitosis and induction of apoptosis in cancer cells. Haspin is a promising therapeutic target in oncology due to its essential role in chromosome segregation. Further in vivo studies are needed to evaluate the compound's efficacy and safety profile.
|
| Enzyme Assay |
In vitro enzyme assays for Haspin-IN-3 involve measuring Haspin kinase activity. The standard protocol includes incubating recombinant Haspin with varying concentrations of Haspin-IN-3 (0.001-1000 nM) and a substrate such as histone H3 or a peptide substrate in the presence of ATP. Phosphorylation is measured using radiometric methods ([³²P]-ATP incorporation), fluorescence-based assays, or by western blot with phospho-specific antibodies (e.g., anti-H3T3ph). IC₅₀ values are calculated from dose-response curves. Selectivity against other kinases is assessed using a panel of kinases.
|
| Cell Assay |
Cell-based assays for Haspin-IN-3 are conducted in cancer cell lines. Cells are treated with Haspin-IN-3 at concentrations ranging from 0.1-1000 nM for 24-72 hours. Histone H3 phosphorylation at threonine 3 (H3T3ph) is analyzed by western blot or immunofluorescence microscopy. Cell cycle analysis is performed by flow cytometry with propidium iodide staining to assess mitotic arrest. Apoptosis is evaluated by Annexin V/PI staining and caspase activation. Cell proliferation and viability are assessed by MTT or CellTiter-Glo assays. Chromosome alignment is examined by immunofluorescence microscopy of mitotic cells.
|
| Animal Protocol |
In vivo animal experiments for Haspin-IN-3 would typically use mouse xenograft models of cancer. Animals would be administered Haspin-IN-3 via oral gavage or intraperitoneal injection at doses determined from PK studies. Tumor volume would be measured periodically, and body weight monitored. At study termination, tumors and tissues would be collected for analysis of H3T3 phosphorylation, mitotic index, proliferation (Ki67), and apoptosis (TUNEL). Pharmacokinetic studies would be performed to determine exposure and bioavailability.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for Haspin-IN-3 are not extensively reported. As a small molecule with a molecular weight of 278.26 g/mol, the compound is expected to have moderate bioavailability. Storage: typically at -20°C. Purity is typically ≥98%. The compound is a potent Haspin inhibitor with an IC₅₀ of 14 nM. Further PK studies would be required for comprehensive characterization.
|
| Toxicity/Toxicokinetics |
Haspin-IN-3 is supplied for research use only and is not intended for human administration. Toxicity data are limited, but the compound is used in cancer research at concentrations that induce mitotic arrest and apoptosis. Standard laboratory safety precautions should be followed. No specific toxicological studies have been published. The compound should be handled with care and stored appropriately.
|
| References | |
| Additional Infomation |
Haspin-IN-3 (CAS 2416569-95-2) is a research compound supplied for laboratory use only. It is not an approved drug and has no clinical trial or marketing authorization status. The compound is a potent Haspin inhibitor with an IC₅₀ of 14 nM. It has anticancer effects. Purity is typically ≥98%. The compound has a molecular formula of C₁₆H₁₀N₂O₃ and a molecular weight of 278.26 g/mol. It is used for research on Haspin biology and cancer.
|
| Molecular Formula |
C16H10N2O3
|
|---|---|
| Molecular Weight |
278.26220369339
|
| Exact Mass |
278.069
|
| CAS # |
2416569-95-2
|
| PubChem CID |
156016477
|
| Appearance |
Light yellow to brown solid powder
|
| LogP |
2.6
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
21
|
| Complexity |
464
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O1C2=CC(O)=CC=C2C(=O)/C/1=C/C1C2=CC=CN=C2NC=1
|
| InChi Key |
VHCZWXXMSGKCKC-NSIKDUERSA-N
|
| InChi Code |
InChI=1S/C16H10N2O3/c19-10-3-4-12-13(7-10)21-14(15(12)20)6-9-8-18-16-11(9)2-1-5-17-16/h1-8,19H,(H,17,18)/b14-6-
|
| Chemical Name |
(2Z)-6-hydroxy-2-(1H-pyrrolo[2,3-b]pyridin-3-ylmethylidene)-1-benzofuran-3-one
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~89.84 mM)
|
|---|---|
| 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 | 3.5938 mL | 17.9688 mL | 35.9376 mL | |
| 5 mM | 0.7188 mL | 3.5938 mL | 7.1875 mL | |
| 10 mM | 0.3594 mL | 1.7969 mL | 3.5938 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
Copyright 2020 InvivoChem LLC | All Rights Reserved
