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| 5mg |
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| Targets |
Rac1‑IN‑4 targets Rac1 (Ras‑related C3 botulinum toxin substrate 1), a small GTPase of the Rho family. Rac1 cycles between an inactive GDP‑bound state and an active GTP‑bound state. Activation of Rac1 promotes actin polymerization, lamellipodia formation, and cell migration, and it is involved in cell proliferation, survival, and gene expression. Rac1 is overexpressed or hyperactivated in many cancers, including breast, colon, pancreatic, and prostate cancers, and is implicated in cancer metastasis. Rac1‑IN‑4 is a selective inhibitor of Rac1, blocking its activation and downstream signaling.
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| ln Vitro |
Rac1‑IN‑4 is a selective inhibitor of Rac1, a Rho GTPase involved in various cellular processes including cytoskeletal dynamics and cell migration. This compound effectively disrupts the signaling pathways mediated by Rac1, making it a valuable tool for studying cancer metastasis and neurodegenerative diseases. Rac1‑IN‑4 inhibits Rac1 activity, leading to reduced cell migration, invasion, and proliferation. No specific IC₅0 values for Rac1 inhibition are reported in the search results. The compound is used to explore the therapeutic potential of targeting Rac1 in cellular signaling and pathology. It is a triazolopyridazine derivative described in a patent (WO2023076259 A1).
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| ln Vivo |
No specific in vivo activity data for Rac1‑IN‑4 are reported in the search results. As a selective Rac1 inhibitor, it has potential for evaluation in animal models of cancer metastasis (e.g., orthotopic breast cancer models, tail vein injection models of lung metastasis) and neurodegenerative diseases (e.g., Alzheimer‘s disease, amyotrophic lateral sclerosis). The compound could be administered orally or intraperitoneally, and endpoints would include tumor growth, metastasis burden, and disease progression. No specific in vivo data are provided.
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| Enzyme Assay |
The binding of Rac1‑IN‑4 to Rac1 is measured by standard biochemical assays using purified recombinant Rac1 protein. A fluorescence polarization (FP) or time‑resolved fluorescence resonance energy transfer (TR‑FRET) assay can be used. A labeled Rac1 ligand or a tracer that binds to the Rac1 active site is used. Rac1‑IN‑4 is added at graded concentrations (0.1‑10,000 nM) to compete for binding, and the IC₅0 is calculated. The inhibition of Rac1 activation can be assessed by measuring Rac1‑GTP levels using a Rac1 activation assay kit (pull‑down with PAK‑PBD). For cellular assays, cancer cell lines (e.g., MDA‑MB‑231 breast cancer, PANC‑1 pancreatic cancer, or HT‑1080 fibrosarcoma) are seeded in 6‑ or 96‑well plates. Cells are treated with Rac1‑IN‑4 at graded concentrations (0.1‑100 microM) for 24‑72 h. Rac1 activation is assessed by measuring GTP‑bound Rac1 levels using a Rac1 activation assay kit. Cell migration is assessed by wound healing (scratch) assay or Transwell migration assay. Cell invasion is assessed using Matrigel‑coated Transwell inserts. Cell viability is measured by MTT or CellTiter‑Glo assays. The IC₅0 for inhibition of migration or proliferation is calculated.
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| Cell Assay |
For in vivo evaluation of anti‑metastatic activity, 6‑8‑week‑old female BALB/c nude mice are injected intravenously (tail vein) with cancer cells (e.g., MDA‑MB‑231 breast cancer) to establish lung metastasis models. Rac1‑IN‑4 would be administered orally or intraperitoneally at doses of 10‑100 mg/kg daily for 2‑4 weeks. At the study endpoint, lungs would be harvested, and metastatic nodules would be counted. For orthotopic tumor models, mice would be injected with cancer cells into the mammary fat pad (for breast cancer) or pancreas, and tumor growth and metastasis would be assessed. No specific protocols are described.
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| Animal Protocol |
Rac1‑IN‑4 (C23H1₆ClN₅O2, MW = 429.86, purity >98%, CAS 2924486‑45‑1) is a solid powder. For storage, the powder should be kept at -20 degC for up to 3 years, sealed and protected from light. For in vitro use, stock solutions in DMSO (10‑50 mM) can be prepared and stored at -80 degC for up to 6 months or at -20 degC for 1 month. For in vivo use, it can be formulated in 10% DMSO / 40% PEG300 / 5% Tween‑80 / 45% saline. No detailed PK parameters are reported.
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| ADME/Pharmacokinetics |
No specific toxicity data for Rac1‑IN‑4 are reported. As a research‑grade Rac1 inhibitor, it is not intended for human or veterinary use. Standard laboratory safety precautions for handling chemicals should be followed. Rac1 is a key regulator of many cellular processes, and its inhibition may have off‑target effects on normal cell function. No LD₅0 or formal toxicology studies are available.
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| Toxicity/Toxicokinetics |
Rac1‑IN‑4 is a research‑grade selective inhibitor of Rac1. Rac1 is a member of the Rho family of small GTPases, which are key regulators of the actin cytoskeleton, cell polarity, and cell migration. Rac1 is a critical driver of cancer metastasis, and its overexpression is associated with poor prognosis in many cancers. Rac1 has also been implicated in neurodegenerative diseases, including Alzheimer‘s disease (where it affects dendritic spine morphology) and amyotrophic lateral sclerosis (ALS). Rac1‑IN‑4 is a triazolopyridazine derivative described in a patent. The compound is for research use only and has not received regulatory approval.
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| References |
| Molecular Formula |
C23H16CLN5O2
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| Molecular Weight |
429.86
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| Exact Mass |
429.099
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| CAS # |
2924486-45-1
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| PubChem CID |
168246389
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| Appearance |
Light yellow to yellow solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
31
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| Complexity |
639
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC=C(O1)C2=NN=C3N2N=C(C=C3)C4=CC(=CC=C4)NC(=O)C5=CC(=CC=C5)Cl
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| InChi Key |
DDIBTZNIAHHIIP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H16ClN5O2/c1-14-8-10-20(31-14)22-27-26-21-11-9-19(28-29(21)22)15-4-3-7-18(13-15)25-23(30)16-5-2-6-17(24)12-16/h2-13H,1H3,(H,25,30)
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| Chemical Name |
3-chloro-N-[3-[3-(5-methylfuran-2-yl)-[1,2,4]triazolo[4,3-b]pyridazin-6-yl]phenyl]benzamide
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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 | 2.3263 mL | 11.6317 mL | 23.2634 mL | |
| 5 mM | 0.4653 mL | 2.3263 mL | 4.6527 mL | |
| 10 mM | 0.2326 mL | 1.1632 mL | 2.3263 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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