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IACS-13909 (IACS 13909; IACS13909) is a novel, potent and specific allosteric inhibitor of SHP2 that suppresses the signaling of RTK/MAPK pathway and overcomes multiple mechanisms underlying osimertinib resistance.
| ln Vitro |
IACS-13909 (10 nM-10 μM; 14 days) treatment can successfully stop wild-type SHP2 and KYSE-520 cells from proliferating [1]. The growth of wild-type SHP2 and KYSE-520 cells is efficiently inhibited by IACS-13909 (1-5 μM; 2 hours) treatment [1]. In a dose-dependent manner, IACS-13909 similarly and efficaciously (GI50 ~1 μM) reduces the proliferation of parental cells and NCI-H1975 CS cells. KYSE-520 cells' pERK and pMEK values [1].
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| ln Vivo |
IACS-13909 (70 mg/kg; sidewall; daily; for 21 days tumor) administration revealed strong tumor growth suppression, with 100% tumor growth inhibition (TGI) reported after 21 days in the scaffold [1].
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| Cell Assay |
Cell Proliferation Assay [1]
Cell Types: Wild-type SHP2 and KYSE-520 Cell Tested Concentrations: 10 nM, 100 nM, 1. 0.041-3.3 μM) inhibits pERK in NCI-H1975 CS cells in a dose-coupled manner [1]. μM, 10 μM Incubation Duration: 14 days Experimental Results: Effectively inhibited cell proliferation. Western Blot Analysis[1] Cell Types: wild-type SHP2 and KYSE-520 Cell Tested Concentrations: 1 μM, 5 μM Incubation Duration: 2 hrs (hours) Experimental Results: Effectively inhibited pERK and pMEK levels. |
| Animal Protocol |
Animal/Disease Models: NSG mice (20-28 g) were injected with KYSE-520 cells [1].
Doses: 70 mg/kg. Route of Administration: oral; daily; lasting for 21 days. Experimental Results: Effectively inhibited tumor growth in mice. |
| References |
| Molecular Formula |
C17H18CL2N6
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|---|---|
| Molecular Weight |
377.271020412445
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| Exact Mass |
376.1
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| Elemental Analysis |
C, 54.12; H, 4.81; Cl, 18.79; N, 22.28
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| CAS # |
2160546-07-4
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| PubChem CID |
132166923
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| Appearance |
White to yellow solid powder
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| LogP |
3
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
25
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| Complexity |
472
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
AMADCPJVPLUGQO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H18Cl2N6/c1-17(20)5-7-25(8-6-17)12-9-21-15-14(23-24-16(15)22-12)10-3-2-4-11(18)13(10)19/h2-4,9H,5-8,20H2,1H3,(H,22,23,24)
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| Chemical Name |
1-[3-(2,3-dichlorophenyl)-2H-pyrazolo[3,4-b]pyrazin-6-yl]-4-methylpiperidin-4-amine
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| Synonyms |
IACS-13909; IACS 13909; IACS13909; BBP-398; BBP 398; BBP398;
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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 : ~10 mg/mL (~26.51 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.65 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 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 + to the above solution and mix evenly; then add 450 μL of 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 | 2.6506 mL | 13.2531 mL | 26.5062 mL | |
| 5 mM | 0.5301 mL | 2.6506 mL | 5.3012 mL | |
| 10 mM | 0.2651 mL | 1.3253 mL | 2.6506 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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