CPI-444 free base · Synonyms: Ciforadenant

Ciforadenant is a potent, orally active and selective adenosine A2A receptor antagonist.

For research use only. Not for human or veterinary use.

Target Adenosine Receptor

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

CPI-444 structure

CAS No.: 1202402-40-1

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
1 g	USD 650.00	BP-01850-1g	Inquire	Get quote
2 g	USD 1,250.00	BP-01850-2g	In stock	Get quote
5 g	USD 2,950.00	BP-01850-5g	In stock	Get quote
10 g	Inquire	BP-01850-10g	Inquire	Inquire

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Description

Ciforadenant (CPI-444) is a potent, orally active and selective adenosine A2A receptor (A2AR) antagonist, which induces antitumor responses.

Biological activity

In Vitro Ciforadenant is a potent, oral, selective A2AR antagonist. CD8+ T cell depletion abrogates the efficacy of Ciforadenant treatment as a single agent as well as in combination with anti-PD-L1, demonstrating a role for CD8+ T cells in mediating primary and secondary immune responses. Anti-tumor efficacy of Ciforadenant±anti-PD-L1 is associated with increased CD8+ cell infiltration and activation in MC38 tumor tissues, and a corresponding rise in PD-1 expression on CD8+ T cells in the spleen. Additionally, levels of immune checkpoints are modulated by treatment with Ciforadenant, including GITR, OX40, and LAG3 on tumor infiltrating lymphocytes and circulating T cells, suggesting a broad role for adenosine mediated immunosuppression. In Vivo Daily treatment of the syngeneic mouse model MC38 with Ciforadenant (1, 10, 100 mg/kg) leads to dose-dependent inhibition of tumor growth, leading to tumor elimination in ~30% of treated mice. Combining Ciforadenant (100 mg/kg, qd, 14 days) with anti-PD-L1 (200 μg, 3qw, 4 doses) treatment in MC38 models synergistically inhibits tumor growth and eliminates tumors in 90% of treated mice. When cured mice are later re-challenged with MC38 cells, tumor growth is rejected in 100% of challenged mice, indicating that Ciforadenant induces systemic anti-tumor immune memory.

Identifiers

SMILES: CC1=CC=C(O1)C1=C2N=NN(CC3=NC(CO[C@H]4CCOC4)=CC=C3)C2=NC(N)=N1
InChIKey: KURQKNMKCGYWRJ-HNNXBMFYSA-N

Specifications

MW (average): 407.4258
Formula: C₂₀H₂₁N₇O₃
CAS No.: 1202402-40-1
Physical state: Solid
Color: White to light yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Stephen Willingham, et al. Abstract PR04: CPI-444: A potent and selective inhibitor of A2AR induces antitumor responses alone and in combination with anti-PD-L1 in preclinical and clinical studies.Cancer Immunoly Research. September 25-28, 2016.

Same target

Search Adenosine Receptor

Same research area

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