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Dalantercept

Cat. No. M24570
Dalantercept Structure
Synonym:

ACE-041

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Quality Control & Documentation
Biological Activity

Dalantercept (ACE-041) is an activin receptor like kinase 1 (ALK1) inhibitor, a ligand trap for bone morphogenetic proteins (BMP) 9 and BMP 10. Dalantercept reduces tumor angiogenesis and delays tumor growth by binding to BMP 9 and BMP 10. As an anti angiogenic agent, Dalantercept has potential applications in persistent or recurrent ovarian cancer, renal cell carcinoma (RCC), and related malignant tumors.

Chemical Information
CAS Number 1186210-24-1
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Ghassan K Abou-Alfa, et al. Oncologist. A Phase Ib, Open-Label Study of Dalantercept, an Activin Receptor-Like Kinase 1 Ligand Trap, plus Sorafenib in Advanced Hepatocellular Carcinoma

[2] Robert A Burger, et al. Gynecol Oncol. Phase II evaluation of dalantercept in the treatment of persistent or recurrent epithelial ovarian cancer: An NRG Oncology/Gynecologic Oncology Group study

[3] Antonio Jimeno, et al. Cancer. A phase 2 study of dalantercept, an activin receptor-like kinase-1 ligand trap, in patients with recurrent or metastatic squamous cell carcinoma of the head and neck

[4] Vicky Makker, et al. Gynecol Oncol. Phase II evaluation of dalantercept, a soluble recombinant activin receptor-like kinase 1 (ALK1) receptor fusion protein, for the treatment of recurrent or persistent endometrial cancer: an NRG Oncology/Gynecologic Oncology Group Study 0229N

[5] Shilpa Gupta, et al. Curr Oncol Rep. Activin receptor inhibitors--dalantercept

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Keywords: Dalantercept, ACE-041 supplier, TGF-beta/Smad, inhibitors, activators


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