[CAS NO. ] Balixafortide TFA

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PRODUCTS SPECIFICATIONS

Catalog

HY-P1682A

Brand

MCE

CAS

-

DESCRIPTION

Overview

MDL	-
Molecular Weight	1978.16
Molecular Formula	C86H119F3N24O23S2
SMILES	-

For research use only. We do not sell to patients.

Summary

Balixafortide TFA (POL6326 TFA) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC ₅₀ < 10 nM. Balixafortide TFA shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7 . Balixafortide TFA blocks β-arrestin recruitment and calcium flux with IC ₅₀ s < 10 nM. Balixafortide TFA is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects ^[1] ^[2] .

IC50 & Target

CXCR4

<10 nM (IC ₅₀ )

In Vitro

Balixafortide potently inhibits pERK / pAKT signaling in the lymphoma lines Namalwa (IC ₅₀ < 200 nM) and Jurkat (IC ₅₀ < 400 nM). Balixafortide efficiently blocks SDF-1 dependent chemotaxis of MDA MB 231 breast cancer cells (IC ₅₀ < 20 nM), Namalwa and Jurkat cells (IC ₅₀ < 10 nM) ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01413568	Polyphor Ltd.	Acute Myeloid Leukemia in Remission\|Adult Acute Lymphoblastic Leukemia in Remission\|Chronic Myelogenous Leukemia (CML)\|Non-Hodgkin´s Lymphoma (NHL) or Hodgkin´s Disease (HD) in 2nd or Greater Complete Remission, Partial Remission\|Chronic Lymphocytic Leukemia (CLL)\|Multiple Myeloma (MM)\|Myelodysplastic Syndrome (MDS)\|Myeloproliferative Disorders	April 2012	Phase 1\|Phase 2
NCT01837095	Polyphor Ltd.	Metastatic Breast Cancer	June 2013	Phase 1
NCT01905475	Polyphor Ltd.	Large Reperfused ST-Elevation Myocardial Infarction	July 2013	Phase 2
NCT01841476	Polyphor Ltd.	Healthy	February 2012	Phase 1
NCT03786094	Polyphor Ltd.	Metastatic Breast Cancer\|Locally Recurrent Breast Cancer	June 14, 2019	Phase 3
NCT01105403	Polyphor Ltd.	Multiple Myeloma	April 2009	Phase 2
NCT04826016	MedSIR	Advanced Breast Cancer	July 2021	Phase 1\|Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture and light

Powder	-80°C	2 years
	-20°C	1 year

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility

In Vitro:

H ₂ O : 100 mg/mL ( 50.55 mM ; Need ultrasonic)

DMSO : 100 mg/mL ( 50.55 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	0.5055 mL	2.5276 mL	5.0552 mL
5 mM	0.1011 mL	0.5055 mL	1.0110 mL
10 mM	0.0506 mL	0.2528 mL	0.5055 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (1.26 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (1.26 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (1.26 mM); Clear solution

* All of the co-solvents are available by MCE.