2. GPCR/G Protein Immunology/Inflammation
  3. CXCR
  4. CXCL-CXCR1/2-IN-1

CXCL-CXCR1/2-IN-1 is an orally active ELR+CXCL-CXCR1/2 pathway inhibitor with an EC50 of 42.7 nM for CXCR2. CXCL-CXCR1/2-IN-1 shows anticancer and antiangiogenic effects.

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CXCL-CXCR1/2-IN-1 Chemical Structure

CXCL-CXCR1/2-IN-1 Chemical Structure

CAS No. : 2415653-55-1

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Based on 1 publication(s) in Google Scholar

CXCL-CXCR1/2-IN-1 Related Antibodies

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Description

CXCL-CXCR1/2-IN-1 is an orally active ELR+CXCL-CXCR1/2 pathway inhibitor with an EC50 of 42.7 nM for CXCR2[1]. CXCL-CXCR1/2-IN-1 shows anticancer and antiangiogenic effects[1].

In Vitro

In renal cell carcinoma (RCC) cell lines (A498, RCC4, 786, and Sunitinib-resistant RCC cell line 786-R) and neck squamous cell carcinoma (HNSCC) cell lines (CAL33, CAL27, Cisplatin- and radiotherapy-resistant cell lines CAL33RR and CAL27RR), CXCL-CXCR1/2-IN-1 (compound 10) shows IC50 values of 2 μM, 2 μM, 2.5 μM, 2 μM, 3 μM, 4 μM, 4 μM, 2.5 μM, and 2.5 μM against A498, RCC4, 786, 786-R, CAL33, CAL27, CAL33RR, and CAL27RR, respectively[1].
CXCL-CXCR1/2-IN-1 inhibits the migration of A498 cancer cells in vitro[1].
CXCL-CXCR1/2-IN-1 (1-2.5 μM; 24-48 h) shows a reduction in the phosphorylation of ERK and AKT in A498 cells. CXCL-CXCR1/2-IN-1 also exhibits the capability to inhibit the secretion of CXCL1, CXCL5, and CXCL8, which are representative proangiogenic ELR+CXCL cytokines[1].

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

CXCL-CXCR1/2-IN-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: A498 cells
Concentration: 2.5 μM
Incubation Time: 24 or 48 h
Result: Showed a reduction in the phosphorylation of ERK and AKT.

RT-PCR[1]

Cell Line: A498 cells
Concentration: 1 or 2.5 μM
Incubation Time: 48 h
Result: Inhibited the levels of CXCL1, CXCL5, CXCL8, and VEGFA mRNA.
In Vivo

CXCL-CXCR1/2-IN-1 (1 μM; 48 h) reduces metastasis area in zebrafish embryos injected with A498 cells[1].
CXCL-CXCR1/2-IN-1 (100 mg/kg; oral gavage; twice a day; for 28 days) inhibits tumor growth in mice[1].

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

Animal Model: Female NOD SCID mice injected with 786 RCC cells[1]
Dosage: 100 mg/kg
Administration: Oral gavage; twice a day; for 28 days
Result: Exhibited remarkable results, with a tumor growth inhibition rate of 87%.
Molecular Weight

383.21

Formula

C14H8Cl2N4O3S
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(NC1=NC2=CC=C([N+]([O-])=O)C=C2S1)NC3=CC(Cl)=CC(Cl)=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 4.17 mg/mL (10.88 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6095 mL 13.0477 mL 26.0954 mL
5 mM 0.5219 mL 2.6095 mL 5.2191 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6095 mL 13.0477 mL 26.0954 mL 65.2384 mL
5 mM 0.5219 mL 2.6095 mL 5.2191 mL 13.0477 mL
10 mM 0.2610 mL 1.3048 mL 2.6095 mL 6.5238 mL
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CXCL-CXCR1/2-IN-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CXCL-CXCR1/2-IN-12415653-55-1CXCRCXC chemokine receptorsC-X-C motif chemokine receptorsanticancerantiangiogenicELR+CXCL-CXCR1/2 pathwayCXCL1CXCL5CXCL8Inhibitorinhibitorinhibit

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