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Taletrectinib free base

Catalog No. T38995 CAS 1505514-27-1

Synonyms: AB-106freebase, Taletrectinib free base, IBI-344 free base, DS-6051b free base

Taletrectinib free base (AB-106 free base) is a novel potent, selective and orally active ROS1/NTRK inhibitor.Taletrectinib free base has potent inhibitory effects on recombinant ROS1, NTRK1, NTRK2, and NTRK3, with IC50s of 0.207, 0.622, 2.28 and 0.98 nM, respectively, Taletrectinib free base also inhibited ROS1 G2032R and other Crizotinib-resistant ROS1 mutations.

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Taletrectinib free base Chemical Structure

Taletrectinib free base, CAS 1505514-27-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 65.00
5 mg	In stock	$ 159.00
10 mg	In stock	$ 255.00
25 mg	In stock	$ 513.00
50 mg	In stock	$ 743.00
100 mg	In stock	$ 1,050.00
1 mL * 10 mM (in DMSO)	In stock	$ 193.00

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Purity: 99.87%

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Description	Taletrectinib free base (AB-106 free base) is a novel potent, selective and orally active ROS1/NTRK inhibitor.Taletrectinib free base has potent inhibitory effects on recombinant ROS1, NTRK1, NTRK2, and NTRK3, with IC50s of 0.207, 0.622, 2.28 and 0.98 nM, respectively, Taletrectinib free base also inhibited ROS1 G2032R and other Crizotinib-resistant ROS1 mutations.
In vitro	Taletrectinib free base (1-1000 nM; 72 h) has an IC50 of ~3 -20 nM against Ba/F3-TPM3-NTRK1, Ba/F3-ETV6-NTRK1, -NTRK2, -NTRK3, or KM12 cells.[1] Taletrectinib free base (0.001-1000 nM; 2 h) dose-dependently inhibits ROS1 autophosphorylation in U-118-MG cells in vitro.[1] Taletrectinib free base potently inhibits ROS1 autophosphorylation in JFCR-165, JFCR-168 and MGH193-1B cells.[1] Taletrectinib free base partially inhibits phosphorylated NTRK1 at 10 nM and completely inhibits it at 100 nM. Taletrectinib free base potently inhibits recombinant ROS1, NTRK1, and NTRK3 in an ATP-competitive manner at subnanomolar concentrations. Taletrectinib free base at 0.2 μM almost completely inhibits ACK, ALK, DDR1, and LTK among the 160 kinases but does not strongly inhibit the other 152 kinases in the presence of 1 mM ATP.[1] Taletrectinib free base effectively inhibits crizotinib-resistant ROS1 secondary mutations, including the G2032R solvent front mutation.[1]
In vivo	Taletrectinib free base (DS-6051b) (25 -200 mg/kg; oral; once daily for 18 days; Balb-c nu/nu mice bearing U-118 MG cells) shows anti-tumor activity.[1] Taletrectinib free base (6.25 -200 mg/kg; oral; once daily for 8 days;) inhibits NTRK-rearranged cancer in Balb-c nu/nu mice harboring KM12 cells.[1] Taletrectinib free base (3-100 mg/kg; p.o.; once daily for 4 days) shows rapid tumor regression in wild-type (WT) and G2032R mutant Ba/F3-carrying mice without severe weight loss.[1]

Synonyms	AB-106freebase, Taletrectinib free base, IBI-344 free base, DS-6051b free base
Molecular Weight	405.47
Formula	C23H24FN5O
CAS No.	1505514-27-1

Storage

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

Solubility Information

DMSO: 55 mg/mL (135.65 mM)

References and Literature

1. Katayama R, et al. The new-generation selective ROS1/NTRK inhibitor DS-6051b overcomes crizotinib resistant ROS1-G2032R mutation in preclinical models. Nat Commun. 2019;10(1):3604. 2. Fujiwara Y, et al. Safety and pharmacokinetics of DS-6051b in Japanese patients with non-small cell lung cancer harboring ROS1 fusions: a phase I study. Oncotarget. 2018;9(34):23729-23737.

Related compound libraries

This product is contained In the following compound libraries：

Tyrosine Kinase Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Drug Repurposing Compound Library Inhibitor Library Kinase Inhibitor Library Bioactive Compound Library Anti-Lung Cancer Compound Library Bioactive Compounds Library Max

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Uniconazole Anti-inflammatory agent 64 Repotrectinib Lorlatinib APG-2449 Merestinib Entrectinib ROS kinases-IN-2

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Keywords

Taletrectinib free base 1505514-27-1 Tyrosine Kinase/Adaptors ROS Kinase AB-106freebase DS-6051b IBI 344 IBI-344 Taletrectinib IBI-344 free base DS-6051b free base IBI344 inhibitor inhibit

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