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KRAS inhibitor-10 manufacturers
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| | KRAS inhibitor-10 Basic information |
| Product Name: | KRAS inhibitor-10 | | Synonyms: | KRAS inhibitor-10;KRAS inhibitor 10,KRAS inhibitor10;2(1H)-Isoquinolinecarboxamide, 7-[2-(3-amino-4-methoxyphenyl)ethoxy]-N-ethyl-3,4-dihydro-6-methoxy-1-(4-methoxy-2-methylphenyl)- | | CAS: | 2578876-75-0 | | MF: | C30H37N3O5 | | MW: | 519.63 | | EINECS: | | | Product Categories: | | | Mol File: | 2578876-75-0.mol |  |
| | KRAS inhibitor-10 Chemical Properties |
| Boiling point | 696.1±55.0 °C(Predicted) | | density | 1.181±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO : 100 mg/mL (192.44 mM; Need ultrasonic) | | form | Solid | | pka | 14.15±0.40(Predicted) | | color | White to off-white |
| | KRAS inhibitor-10 Usage And Synthesis |
| Uses | KRAS inhibitor-10 selectively and effectively inhibit RAS proteins, and particularly KRAS proteins. KRAS inhibitor-10 is an orally active anti-cancer agent and can be used for cancer research, such as pancreatic cancer, breast cancer, multiple myeloma, leukemia and lung cancer. KRAS inhibitor-10 is atetrahydroisoquinoline compound (compound 11) extracted from patent WO2021005165 A1[1]. | | Biological Activity | KRAS inhibitor-10 selectively and effectively inhibit RAS proteins, and particularly KRAS proteins. KRAS inhibitor-10 is an orally active anti-cancer agent and can be used for cancer research, such as pancreatic cancer, breast cancer, multiple myeloma, leukemia and lung cancer. KRAS inhibitor-10 is a tetrahydroisoquinoline compound (compound 11) extracted from patent WO2021005165 A1[1].
KRAS inhibitor-10 (0.1-50 μμ; 72 hours) has antiproliferative effects in KRas mutant tumor cells, KRAS inhibitor-10 is against A549 (lung carcinoma cell line bearing KRasG12S oncogenic mutation), H358 (non-small cell lung cancer line bearing KRasG12C oncogenic mutation), PANC-1 (epithelioid carcinoma of the pancreas cell line bearing KRasG12D oncogenic mutation) and RPMI (myeloma cell line bearing KRasG12A oncogenic mutation) cell proliferation with IC50 values of 0.2 μM, 0.2 μM, 0.1 μM and 0.8 μM, respectively[1].KRAS inhibitor-10 (0-1 μM, 7 days) is against cell viability in a 3D CellTiter-GloTM cell viability assay for NIH-H358 cell, the IC50 value is 0.413 μM[1].
KRAS inhibitor-10 (oral administration; 20 mg/kg; BID; 27 days) is safe and tolerate for the bearing mice. KRAS inhibitor-10 demonstrates significant oral anti-tumor activities in vivo. And the tumor growth inhibition (TGI) value is 48.22% for KRAS inhibitor-10[1]. | | in vivo | KRAS inhibitor-10 (oral administration; 20 mg/kg; BID; 27 days) is safe and tolerate for the bearing mice. KRAS inhibitor-10 demonstrates significant oral anti-tumor activities in vivo. And the tumor growth inhibition (TGI) value is 48.22% for KRAS inhibitor-10[1]. | Animal Model: | Subcutaneous NCI-H358 Human Lung Cancer Model in NCr nude mice[1] | | Dosage: | 20 mg/kg | | Administration: | Oral administration; 20 mg/kg; BID; 27 days | | Result: | Decreased tumor volume and exhibited anti-tumor effects in the bearing mice. |
| | IC 50 | KRas G12C | | References | [1]. Miguel VEGA GARCíA, et al. Tetrahydroisoquinoline compounds. Patent wo2021002165 |
| | KRAS inhibitor-10 Preparation Products And Raw materials |
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