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COTI-2

Cat. No. M13551
COTI-2 Structure
Size Price Availability Quantity
5mg USD 80  USD80 In stock
10mg USD 130  USD130 In stock
25mg USD 240  USD240 In stock
50mg USD 360  USD360 In stock
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Quality Control & Documentation
Biological Activity

COTI-2, an anti-cancer drug with low toxicity, is an orally available third generation activator of p53 mutant forms. COTI-2 acts both by reactivating mutant p53 and inhibiting the PI3K/AKT/mTOR pathway. COTI-2 induces apoptosis in multiple human tumor cell lines. COTI-2 exhibits antitumor activity in HNSCC through p53-dependent and -independent mechanisms. COTI-2 converts mutant p53 to wild-type conformation.

Chemical Information
Molecular Weight 366.48
CAS Number 1039455-84-9
Solubility (25°C) DMSO 5 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Yingmeng Guo, et al. Bioengineered. COTI-2 induces cell apoptosis in pediatric acute lymphoblastic leukemia via upregulation of miR-203

[2] Naoise C Synnott, et al. Breast Cancer Res Treat. COTI-2 reactivates mutant p53 and inhibits growth of triple-negative breast cancer cells

[3] Antje Lindemann, et al. Clin Cancer Res. COTI-2, A Novel Thiosemicarbazone Derivative, Exhibits Antitumor Activity in HNSCC through p53-dependent and -independent Mechanisms

[4] Raman Preet Kaur, et al. Curr Pharm Des. Role of p53 Gene in Breast Cancer: Focus on Mutation Spectrum and Therapeutic Strategies

[5] Michael J Duffy, et al. Eur J Cancer. Mutant p53 as a target for cancer treatment

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Keywords: COTI-2 supplier, p53, inhibitors, activators


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