R1530
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MedKoo CAT#: 202391

CAS#: 882531-87-5

Description: R1530 is a pyrazolobenzodiazepine small molecule with potential antiangiogenesis and antineoplastic activities. 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.


Price and Availability

Size Price Shipping out time Quantity
10mg USD 190 Same day
25mg USD 250 Same day
50mg USD 450 Same day
100mg USD 850 Same day
200mg USD 1250 Same day
500mg USD 2150 Same day
1g USD 2950 2 weeks
2g USD 3950 2 weeks
Inquire bulk and customized quantity

Pricing updated 2020-08-03. Prices are subject to change without notice.

R1530, purity > 98%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 200mg may be 2 weeks.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 202391
Name: R1530
CAS#: 882531-87-5
Chemical Formula: C18H14ClFN4O
Exact Mass: 356.08402
Molecular Weight: 356.78136
Elemental Analysis: C, 60.60; H, 3.96; Cl, 9.94; F, 5.32; N, 15.70; O, 4.48


Synonym: R1530; R-1530; R 1530.

IUPAC/Chemical Name: 5-(2-chlorophenyl)-7-fluoro-8-methoxy-3-methyl-2,10-dihydrobenzo[e]pyrazolo[4,3-b][1,4]diazepine

InChi Key: UOVCGJXDGOGOCZ-UHFFFAOYSA-N

InChi Code: InChI=1S/C18H14ClFN4O/c1-9-16-18(24-23-9)21-14-8-15(25-2)13(20)7-11(14)17(22-16)10-5-3-4-6-12(10)19/h3-8H,1-2H3,(H2,21,23,24)

SMILES Code: CC1=C2N=C(C3=CC=CC=C3Cl)C4=CC(F)=C(OC)C=C4NC2=NN1


Technical Data

Appearance:
white solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (SDS):

Shipping Condition:
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 Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001


Additional Information

 
Preclinical study of R1350 (data published in 2011): Reclinical study showed that R1530 strongly inhibited human tumor cell proliferation. Growth factor-driven proliferation of endothelial and fibroblast cells was also inhibited. 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. R1530 has demonstrated activity against a range of tumor models in vitro and in vivo and is an effective inhibitor of angiogenesis. These findings support the approach of targeting multiple pathways in the search for potential agents with improved anticancer properties. (source: Cancer Chemother Pharmacol. 2011 Dec;68(6):1585-94.).
 
         


References