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ANG1005

Cat. No. M31338
ANG1005 Structure
Synonym:

Paclitaxel trevatide

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Quality Control & Documentation
Biological Activity

ANG1005 is a paclitaxel derivative as well as a peptide-coupled compound (PDC) consisting of three paclitaxel and Angiopep-2 covalently linked. In addition, ANG1005 is a modulator of LDLR and an inhibitor of mitosis and microtubule proteins.

Chemical Information
Molecular Weight 5127.33
Formula C256H306N32O81
CAS Number 1075214-55-9
Form Solid
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] Priya Kumthekar, et al. Clin Cancer Res. ANG1005, a Brain-Penetrating Peptide-Drug Conjugate, Shows Activity in Patients with Breast Cancer with Leptomeningeal Carcinomatosis and Recurrent Brain Metastases

[2] Fei Li, et al. Genes Dis. Targeting metastatic breast cancer with ANG1005, a novel peptide-paclitaxel conjugate that crosses the blood-brain-barrier (BBB)

[3] C C O'Sullivan, et al. Breast Cancer Res Treat. ANG1005 for breast cancer brain metastases: correlation between 18F-FLT-PET after first cycle and MRI in response assessment

[4] Fancy C Thomas, et al. Pharm Res. Uptake of ANG1005, a novel paclitaxel derivative, through the blood-brain barrier into brain and experimental brain metastases of breast cancer

[5] A Régina, et al. Br J Pharmacol. Antitumour activity of ANG1005, a conjugate between paclitaxel and the new brain delivery vector Angiopep-2

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Keywords: ANG1005, Paclitaxel trevatide supplier, inhibitors, activators


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