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Tafetinib

Catalog No. T28911 CAS 1032265-57-8

Synonyms: SIM-010603, SIM010603, SIM 010603

Tafetinib (SIM-010603) is a novel potent and orally available tyrosine kinase inhibitor with anti-angiogenic and anti-tumour activity.

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Tafetinib, CAS 1032265-57-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 250.00
5 mg	In stock	$ 623.00
10 mg	In stock	$ 887.00
25 mg	In stock	$ 1,330.00
50 mg	In stock	$ 1,780.00
100 mg	In stock	$ 2,430.00
500 mg	In stock	$ 4,880.00

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Purity: 96.66%

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Description

Tafetinib (SIM-010603) is a novel potent and orally available tyrosine kinase inhibitor with anti-angiogenic and anti-tumour activity.

In vivo

SIM010603, a promising multi-targeted receptor tyrosine kinase (RTK) inhibitor, is now being considered for evaluation in a phase clinical trial. In this work, the subchronic toxicity of SIM010603 in SD rats and beagle dogs has been characterized. Rats and dogs received SIM010603 orally (0-20 and 0-10mg/kg/day, respectively) on a consecutive daily dosing schedule for 28 days following a 14-day recovery period. Sunitinib was used as a positive control. The No Observed Adverse Effect Level (NOAEL) of SIM010603 was 5mg/kg/day for rats, and undefined for dogs. The treatment resulted in unscheduled mortality in dogs receiving 10mg/kg of SIM010603 or Sunitinib. The adverse effects of SIM010603 on rats and dogs mainly included gastrointestinal toxicity, skeletal toxicity, myelosuppression, thymus atrophy, bronchopneumonia, cardiovascular dysfunction, and pancreatic toxicity. Similar observations have also been noted with this class of RTK signaling inhibitors and are consistent with pharmacologic perturbations of physiologic/angiogenic processes associated with the intended molecular targets. Most treatment-induced effects were reversible or showed ongoing recovery upon discontinuation of treatment. SIM010603 has shown a comparable toxicity effect on beagle dogs, while better tolerability on SD rats when compared to Sunitinib.[2]

Synonyms	SIM-010603, SIM010603, SIM 010603
Molecular Weight	424.51
Formula	C24H29FN4O2
CAS No.	1032265-57-8

Storage

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

References and Literature

1. Shao F, et al. Simultaneous quantification of tafetinib (SIM010603), a novel potent inhibitor of receptor tyrosine kinase, and its major metabolite in dog plasma by HPLC-ESI/MS/MS and its application to a pharmacokinetic study. J Pharm Biomed Anal. 2013 Jul-Aug;81-82:50-5. 2. Mao Y, et al. Evaluation of subchronic toxicity of SIM010603, a potent inhibitor of receptor tyrosine kinase, after 28-day repeated oral administration in SD rats and beagle dogs. Food Chem Toxicol. 2012 May;50(5):1256-70. 3. Wang D, et al. Preclinical anti-angiogenesis and anti-tumor activity of SIM010603, an oral, multi-targets receptor tyrosine kinases inhibitor. Cancer Chemother Pharmacol. 2012 Jan;69(1):173-8

Related compound libraries

This product is contained In the following compound libraries：

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

Related Products

Related compounds with same targets

Decernotinib Tyk2-IN-3 Alectinib Cerdulatinib GTP-14564 Filgotinib AMG 900 Vecabrutinib

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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

Tafetinib 1032265-57-8 Tyrosine Kinase/Adaptors Tyrosine Kinases SIM-010603 SIM010603 SIM 010603 inhibitor inhibit

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