Balixafortide(POL6326) Datasheet | DC21522

Balixafortide(POL6326) — Datasheet

CAT. NO. DC21522

Parameter	Value
Chemical Name	Ala-cys-ser-ala-pro-arg-tyr-cys-tyr-gln-lys-pro-pro-tyr-his cyclic (2->9)-disulfide
CAS No.	1051366-32-5
Synonyms	POL6326;POL-6326
Formula	C84H118N24O21S2
M.Wt	1864.11
SMILES	C[C@@H]1NN[C@@H](CC2NC=NC=2)C(=O)N[C@@H](CC2C=CC(O)=CC=2)C(=O)N2[C@@H](CCC2)C(=O)N2[C@H](CCC2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC2C=CC(O)=CC=2)C(=O)N[C@@H]2C(N[C@@H](CC3C=CC(O)=CC=3)C(C([C@H](CCCNC(N)=N)NC([C@H](CCN)NC([C@@H]3N(C([C@H](C)NC([C@H](CO)NC(=O)[C@H](CSSC2)NC1=O)=O)=O)CCC3)=O)=O)=O)=O)=O
Purity	>98%
Storage	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects[1][2].

In Vitro

Balixafortide potently inhibits pERK / pAKT signaling in the lymphoma lines Namalwa (IC50< 200 nM) and Jurkat (IC50 < 400 nM). Balixafortide efficiently blocks SDF-1 dependent chemotaxis of MDA MB 231 breast cancer cells (IC50 < 20 nM), Namalwa and Jurkat cells (IC50 < 10 nM)[1].

In Vivo

Balixafortide is optimized for favorable mouse absorption, distribution, metabolism and excretion (ADME) properties with balanced plasma protein binding, greater plasma and microsomal stability[1].

Target

CXCR4:<10 nM (IC50)

References & source

[1]. Zimmermann J, et al. Anti-tumor cell activity and in vitro profile of the next generation CXCR4 antagonist Balixafortide. Ann Oncol. 2018 Oct;29 Suppl 8:viii103.

[2]. Karpova D, et al. Mobilization of hematopoietic stem cells with the novel CXCR4 antagonist POL6326 (balixafortide) in healthy volunteers-results of a dose escalation trial. J Transl Med. 2017 Jan 3;15(1):2.

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.