| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
KRAS mutant tumor cells are inhibited in their ability to proliferate by KRAS inhibitor-10 (0.1-50μM; 72 hours). KRAS inhibitor-10 specifically targets A549, a lung cancer cell line with an oncogenic KRasG12S mutation, and H358, a non-small cell line with the same mutation. The KRasG12C oncogenic mutation in lung cancer cell line, the KRasG12D oncogenic mutation in pancreatic epithelioid carcinoma cell line PANC-1, and the KRasG12A oncogenic mutation in myeloma cell line RPMI all had IC50 values of 0.2 μM, 0.2 μM, 0.1 μM, and 0.8 μM, respectively, for cell proliferation [1]. In the 3D CellTiter-GloTM cell viability experiment of NIH-H358 cells, KRAS inhibitor-10 (0-1 μM, 7 days) inhibited cell viability with an IC50 value of 0.413 μM [1].
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|---|---|
| ln Vivo |
KRAS inhibitor-10 (oral; 20 mg/kg; BID; 27 days) is safe and well tolerated in pregnant mice. KRAS inhibitor-10 showed substantial oral anticancer efficacy in vivo. The tumor growth inhibition (TGI) value of KRAS inhibitor 10 is 48.22% [1].
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| Animal Protocol |
Animal/Disease Models: NCr nude mice subcutaneously (sc) (sc) injected NCI-H358 human lung cancer model [1]
Doses: 20 mg/kg Route of Administration: oral; Route of Administration: oral. 20 mg/kg; bid; 27-day Experimental Results: Tumor volume in tumor-bearing mice diminished and anti-tumor effects were demonstrated. |
| References |
| Molecular Formula |
C30H37N3O5
|
|---|---|
| Molecular Weight |
519.63
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| Exact Mass |
519.273
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| CAS # |
2578876-75-0
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| PubChem CID |
155471755
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| Appearance |
White to off-white solid powder
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| LogP |
4.7
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
38
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| Complexity |
741
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1C(C)=C(C=CC=1OC)C1C2=CC(=C(OC)C=C2CCN1C(NCC)=O)OCCC1C=CC(OC)=C(N)C=1
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| InChi Key |
WKOOIGPIJNQBPY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C30H37N3O5/c1-6-32-30(34)33-13-11-21-17-27(37-5)28(38-14-12-20-7-10-26(36-4)25(31)16-20)18-24(21)29(33)23-9-8-22(35-3)15-19(23)2/h7-10,15-18,29H,6,11-14,31H2,1-5H3,(H,32,34)
|
| Chemical Name |
7-[2-(3-amino-4-methoxyphenyl)ethoxy]-N-ethyl-6-methoxy-1-(4-methoxy-2-methylphenyl)-3,4-dihydro-1H-isoquinoline-2-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 : ~100 mg/mL (~192.44 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.81 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.81 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9244 mL | 9.6222 mL | 19.2445 mL | |
| 5 mM | 0.3849 mL | 1.9244 mL | 3.8489 mL | |
| 10 mM | 0.1924 mL | 0.9622 mL | 1.9244 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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