1. Protein Tyrosine Kinase/RTK
  2. VEGFR

R1530 

Cat. No.: HY-13737 Purity: 98.73%
Handling Instructions

R1530 is the multikinase inhibitor with potential antiangiogenesis and antineoplastic activities.

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

R1530 Chemical Structure

R1530 Chemical Structure

CAS No. : 882531-87-5

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 138 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
10 mg USD 125 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

View All VEGFR Isoform Specific Products:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

R1530 is the multikinase inhibitor with potential antiangiogenesis and antineoplastic activities. IC50 Value: Target: VEGFR; PDGFR R1530 is also a mitosis-angiogenesis inhibitor (MAI) that inhibits multiple receptor tyrosine kinases involved in angiogenesis, such as vascular endothelial growth factor receptor (VEGFR)-1, -2, -3, platelet-derived growth factor receptor (PDGFR) beta? FMS-like tyrosine kinase (Flt)-3, and fibroblast growth factor receptor (FGFR) -1, -2. In addition, this agents exhibits anti-proliferative activity by initiating mitotic arrest and inducing apoptosis. in vitro: In the presence of R1530, polyploid cancer cells underwent apoptosis or became senescent which translated into potent in vitro and in vivo efficacy. Normal proliferating cells were resistant to R1530-induced polyploidy thus supporting the rationale for cancer therapy by induced polyploidy. Mitotic checkpoint kinase BubR1 was found downregulated during R1530-induced exit from mitosis, a likely consequence of PLK4 inhibition [1]. R1530 strongly inhibited human tumor cell proliferation. Growth factor-driven proliferation of endothelial and fibroblast cells was also inhibited [2]. in vivo: Significant tumor growth inhibition was demonstrated in a lung cancer xenograft model with a range of once daily, weekly and twice-weekly doses of R1530 (3.125-50 mg/kg qd, 100 mg/kg qw, 100 mg/kg biw). Daily doses were most effective in the lung cancer model and also had significant growth inhibitory effects in models of colorectal, prostate, and breast tumors. Tumor regression occurred in all models treated with the maximum tolerated daily dose (50 mg/kg). The doses of 25 and 50 mg/kg qd resulted in biologically significant increased survival in all tested models. After oral administration in nude mice, R1530 showed good tissue penetration. Exposure was dose dependent up to 100 mg/kg with oral administration [2]. Toxicity: N/A Clinical trial: A Multiple Ascending Dose Study of R-1530 in Patients With Advanced Solid Tumors. Phase 1

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.8028 mL 14.0142 mL 28.0285 mL
5 mM 0.5606 mL 2.8028 mL 5.6057 mL
10 mM 0.2803 mL 1.4014 mL 2.8028 mL
Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

356.78

Formula

C₁₈H₁₄ClFN₄O

CAS No.

882531-87-5

SMILES

CC(NN1)=C2C1=NC3=CC(OC)=C(F)C=C3C(C4=CC=CC=C4Cl)=N2

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 53 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 98.73%

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
R1530
Cat. No.:
HY-13737
Quantity: