KRAS inhibitor-10 - 10mM in DMSO, high purity , CAS No.2578876-75-0(DMSO)

Item Number

K654855

• Specifications & Purity: 10mM in DMSO
• Storage Temp: Store at -80°C
• Shipped In: Ice chest + Ice pads

Product Description

KRAS inhibitor-10 (compound 11) 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

In Vitro

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 KRas G12S oncogenic mutation), H358 (non-small cell lung cancer line bearing KRas G12C oncogenic mutation), PANC-1 (epithelioid carcinoma of the pancreas cell line bearing KRas G12D oncogenic mutation) and RPMI (myeloma cell line bearing KRas G12A oncogenic mutation) cell proliferation with IC 50 values of 0.2 μM, 0.2 μM, 0.1 μM and 0.8 μM, respectively. 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 IC 50 value is 0.413 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Subcutaneous NCI-H358 Human Lung Cancer Model in NCr nude mice 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.

IC50& Target:KRas G12C