Taletrectinib free base Biochemical

Taletrectinib free base

Cat. Num. AAA227767

• Purity: 98%
• Synonyms: Taletrectinib free base; N/A; Taletrectinib free base biochemical

• Purity/Purification: 98%

• CAS: 1505514-27-1
• Solubility: <1mg/ml refers to the product slightly soluble or insoluble
• In vitro: Taletrectinib (DS-6051b) free base (25-200 mg/kg; p.o.; once daily for 18 days) shows antitumor activity[1]. Taletrectinib free base (6.25-200mg/kg; p.o.; once daily for 8 days) inhibits NTRK-rearranged cancer in Balb-c nu/nu mice bearing KM12 cells[1]. Taletrectinib free base (3-100 mg/kg; p.o.; once daily for 4 days) shows rapid tumor regression in the wild-type (WT) and the G2032R-mutant Ba/F3-bearing mice without severe body weight loss[1]. Animal Model: Balb-c nu/nu mice (bearing U-118 MG cells)[1]. Dosage: 25, 50, 100, and 200mg/kg. Administration: P.o.; once daily for 18 days. Result: Effectively inhibited tumor growth at >=25mg/kg without significant body weight loss.
• Preparation and Storage: Powder: -20 degree C for 3 years; In solvent: -80 degree C for 2 years

Structure

(NCT-501 hydrochloride, CAS 2080306-22-3)

Structure

(NCT-501 hydrochloride, CAS 2080306-22-3)

Related Product Information for Taletrectinib free base biochemical

Taletrectinib (DS-6051b) free base is a potent, orally active, and next-generation selective ROS1/NTRK inhibitor. Taletrectinib free base potently inhibits recombinant ROS1, NTRK1, NTRK2, and NTRK3 with IC 50 s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib free base also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants.

References

1. Kulsum S et al. Cancer stem cell mediated acquired chemoresistance in head and neck cancer can be abrogated by Aldehydedehydrogenase 1 A1 inhibition.
2. Yang SM, et al. Discovery of NCT-501, a Potent and Selective Theophylline-Based Inhibitor of Aldehyde Dehydrogenase 1A1(ALDH1A1). J Med Chem. 2015 Aug 13;58(15):5967-5978.