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KRAS inhibitor-10

Catalog No. T36761 CAS 2578876-75-0

KRAS inhibitor-10 (WO2021005165 A1, compound 11) is a potent and selective inhibitor of RAS proteins, with a specific focus on KRAS proteins. This orally active anti-cancer agent demonstrates strong efficacy in cancer research, specifically in pancreatic cancer, breast cancer, multiple myeloma, leukemia, and lung cancer. KRAS inhibitor-10 is classified as a tetrahydroisoquinoline compound. Its inhibitory properties provide valuable insights and potential therapeutic applications in the field of oncology [1].

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KRAS inhibitor-10, CAS 2578876-75-0

Pack Size	Availability	Price/USD
25 mg	6-8 weeks	$ 1,520.00
50 mg	6-8 weeks	$ 1,980.00
100 mg	6-8 weeks	$ 2,500.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

Storage & Solubility Information

Description	KRAS inhibitor-10 (WO2021005165 A1, compound 11) is a potent and selective inhibitor of RAS proteins, with a specific focus on KRAS proteins. This orally active anti-cancer agent demonstrates strong efficacy in cancer research, specifically in pancreatic cancer, breast cancer, multiple myeloma, leukemia, and lung cancer. KRAS inhibitor-10 is classified as a tetrahydroisoquinoline compound. Its inhibitory properties provide valuable insights and potential therapeutic applications in the field of oncology [1].
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 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].
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].

Molecular Weight	519.63
Formula	C30H37N3O5
CAS No.	2578876-75-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (192.44 mM), Sonication is recommended.

References and Literature

1. Miguel VEGA GARCíA, et al. Tetrahydroisoquinoline compounds. Patent wo2021002165

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid 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 master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

KRAS inhibitor-10 2578876-75-0 KRAS inhibitor 10 KRAS inhibitor10 inhibitor inhibit

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