| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Other Sizes |
Purity: ≥98%
| Targets |
SAR348830 targets anaplastic lymphoma kinase (ALK), a receptor tyrosine kinase that is frequently mutated, amplified, or rearranged in various cancers, including non-small cell lung cancer, neuroblastoma, and anaplastic large cell lymphoma. ALK activation promotes cell proliferation, survival, and migration through downstream signaling pathways including PI3K/AKT, RAS/MAPK, and JAK/STAT. By inhibiting ALK kinase activity, SAR348830 blocks these signaling pathways, leading to cell cycle arrest and apoptosis in ALK-dependent cancer cells. The compound is a potent and selective inhibitor of ALK.
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| ln Vitro |
In vitro, SAR348830 acts as a potent and selective inhibitor of ALK kinase activity. The compound's ability to inhibit ALK has been demonstrated in kinase activity assays using recombinant ALK protein. SAR348830 inhibits the phosphorylation of ALK and its downstream substrates in ALK-dependent cancer cell lines. The compound shows selectivity for ALK over other kinases, although specific IC50 values are not extensively reported in the available literature. SAR348830 inhibits cell proliferation and induces apoptosis in ALK-dependent cancer cells.
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| ln Vivo |
In vivo, SAR348830 has been evaluated for its anti-tumor efficacy in preclinical models of ALK-driven cancers. The compound has the potential to be used for treating non-small cell lung cancer. However, specific in vivo experimental details are not extensively reported in the available literature. As a potent and selective ALK inhibitor, SAR348830 is expected to demonstrate tumor growth inhibition in xenograft models of ALK-dependent cancers. Further in vivo studies would be required to fully characterize its efficacy and safety.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for SAR348830 are kinase activity assays using purified recombinant ALK protein. The enzyme is incubated with a peptide substrate and ATP in the presence of varying concentrations of SAR348830, and the extent of substrate phosphorylation is measured using methods such as luminescence, fluorescence, or radioactivity. The IC50 for inhibition of ALK kinase activity is determined from dose-response curves. Selectivity is assessed by testing the compound against a panel of other kinases. These assays confirm the compound's direct inhibition of ALK.
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| Cell Assay |
In vitro cellular assays for SAR348830 are performed using ALK-dependent cancer cell lines, such as H3122 or Karpas-299 cells. Cells are treated with varying concentrations of SAR348830, and cell viability is measured using MTT or CellTiter-Glo assays. The phosphorylation of ALK and its downstream substrates (e.g., AKT, ERK, STAT3) is assessed by Western blotting. Cell cycle distribution is analyzed by flow cytometry, and apoptosis is evaluated using annexin V staining or caspase activity assays. These assays confirm the compound's ability to inhibit ALK signaling in cells.
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| Animal Protocol |
In vivo animal experiments for SAR348830 are conducted in xenograft mouse models of ALK-dependent cancers. Immunocompromised mice are implanted with human tumor cell lines (e.g., H3122 NSCLC cells) and treated with SAR348830 via oral or intraperitoneal administration. Tumor growth inhibition is monitored, and endpoints include tumor volume, tumor weight, and survival. Pharmacodynamic markers such as ALK phosphorylation in tumor tissues are assessed by immunohistochemistry or Western blotting. These studies evaluate the compound's anti-tumor efficacy.
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| ADME/Pharmacokinetics |
SAR348830 has a molecular weight of 537.65 g/mol and a molecular formula of C28H32FN5O3S. The compound is soluble in DMSO at concentrations up to 25 mg/mL (46.5 mM). For in vivo administration, it can be formulated in 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline at concentrations up to 2 mg/mL (3.72 mM). The compound is stable as a powder at -20°C for up to 3 years and in solution at -80°C for up to 1 year.
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| Toxicity/Toxicokinetics |
The toxicological profile of SAR348830 has not been extensively characterized in publicly available literature. As a kinase inhibitor, SAR348830 may have potential off-target effects and toxicity to normal cells. Standard toxicology studies, including assessment of cytotoxicity in normal cell lines and acute and subchronic toxicity in animal models, would be necessary to establish its safety profile. The compound's selectivity for ALK over other kinases suggests a reduced risk of off-target effects, but comprehensive toxicity testing is not available.
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| References | |
| Additional Infomation |
SAR348830 is a potent and selective inhibitor of anaplastic lymphoma kinase (ALK) with potential for treating non-small cell lung cancer. It is also known as ALK kinase inhibitor-1 and is derived from patent literature US20130261106A1. The compound has a thieno[3,2-d]pyrimidine core structure. SAR348830 is a research compound used for studying ALK-driven cancers and is not an approved drug. Further preclinical and clinical development would be required to establish its therapeutic utility.
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| Molecular Formula |
C28H32FN5O3S
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|---|---|
| Molecular Weight |
537.648788452148
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| Exact Mass |
537.221
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| Elemental Analysis |
C, 62.55; H, 6.00; F, 3.53; N, 13.03; O, 8.93; S, 5.96
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| CAS # |
1462949-64-9
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| Related CAS # |
1462949-64-9
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| PubChem CID |
86698062
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
735.9±70.0 °C at 760 mmHg
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| Flash Point |
398.8±35.7 °C
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| Vapour Pressure |
0.0±2.5 mmHg at 25°C
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| Index of Refraction |
1.646
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| LogP |
4.32
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
38
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| Complexity |
747
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1C(CO)=C(C2C=C(C=CC=2OC)F)C2=C1C=NC(=N2)NC1C=CC(=CC=1OC(C)C)N1CCN(C)CC1
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| InChi Key |
SWRGFJBGNAEJOY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H32FN5O3S/c1-17(2)37-23-14-19(34-11-9-33(3)10-12-34)6-7-21(23)31-28-30-15-24-27(32-28)26(25(16-35)38-24)20-13-18(29)5-8-22(20)36-4/h5-8,13-15,17,35H,9-12,16H2,1-4H3,(H,30,31,32)
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| Chemical Name |
[7-(5-fluoro-2-methoxyphenyl)-2-[4-(4-methylpiperazin-1-yl)-2-propan-2-yloxyanilino]thieno[3,2-d]pyrimidin-6-yl]methanol
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| Synonyms |
SAR348830; SAR-348830; SAR 348830
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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 (~186.0 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.65 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 25.0 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 | 1.8599 mL | 9.2997 mL | 18.5995 mL | |
| 5 mM | 0.3720 mL | 1.8599 mL | 3.7199 mL | |
| 10 mM | 0.1860 mL | 0.9300 mL | 1.8599 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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