CAS 882531-87-5|R1530

Introduction：Basic information about CAS 882531-87-5|R1530, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. R1530 BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Articles1
6. Synonyms

Common Name	R1530
CAS Number	882531-87-5	Molecular Weight	356.781
Density	1.5±0.1 g/cm3	Boiling Point	496.4±55.0 °C at 760 mmHg
Molecular Formula	C₁₈H₁₄ClFN₄O	Melting Point	/
MSDS	ChineseUSA	Flash Point	254.0±31.5 °C
Symbol	GHS07	Signal Word	Warning

Names

Name	5-(2-chlorophenyl)-7-fluoro-8-methoxy-3-methyl-1,2-dihydropyrazolo[3,4-b][1,4]benzodiazepine
Synonym	More Synonyms

R1530 BiologicalActivity

Description	R1530 is the multikinase inhibitor with potential antiangiogenesis and antineoplastic activities. IC50 Value: Target: VEGFR; PDGFRR1530 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: /Clinical trial: A Multiple Ascending Dose Study of R-1530 in Patients With Advanced Solid Tumors. Phase 1
Related Catalog	Research Areas >>Cancer
References	[1]. Tovar C, et al. Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: Implications for therapy. Cell Cycle. 2010 Aug 15;9(16):3364-75. [2]. Kolinsky K, et al. Preclinical evaluation of the novel multi-targeted agent R1530. Cancer Chemother Pharmacol. 2011 Dec;68(6):1585-94.

Description

R1530 is the multikinase inhibitor with potential antiangiogenesis and antineoplastic activities. IC50 Value: Target: VEGFR; PDGFRR1530 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: /Clinical trial: A Multiple Ascending Dose Study of R-1530 in Patients With Advanced Solid Tumors. Phase 1

Related Catalog

Research Areas >>Cancer

References

[1]. Tovar C, et al. Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: Implications for therapy. Cell Cycle. 2010 Aug 15;9(16):3364-75.

[2]. Kolinsky K, et al. Preclinical evaluation of the novel multi-targeted agent R1530. Cancer Chemother Pharmacol. 2011 Dec;68(6):1585-94.

Chemical & Physical Properties

Density	1.5±0.1 g/cm3
Boiling Point	496.4±55.0 °C at 760 mmHg
Molecular Formula	C₁₈H₁₄ClFN₄O
Molecular Weight	356.781
Flash Point	254.0±31.5 °C
Exact Mass	356.084015
PSA	66.59000
LogP	3.34
Vapour Pressure	0.0±1.3 mmHg at 25°C
Index of Refraction	1.687
InChIKey	UOVCGJXDGOGOCZ-UHFFFAOYSA-N
SMILES	COc1cc2c(cc1F)C(c1ccccc1Cl)=Nc1c(n[nH]c1C)N2
Storage condition	2-8℃

Safety Information

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H315-H319-H335
Precautionary Statements	P261-P305 + P351 + P338
RIDADR	NONH for all modes of transport

Articles1

A two-stage combined trickle bed reactor/biofilter for treatment of styrene/acetone vapor mixtures.

J. Environ. Sci. Health. A. Tox. Hazard. Subst. Environ. Eng. 50 , 1148-59, (2015)

Performance of a two-stage biofiltration system was investigated for removal of styrene-acetone mixtures. High steady-state acetone loadings (above C(in)(Ac) = 0.5 g.m(-3) corresponding to the loading...

Synonyms

Pyrazolo(3,4-b)(1,4)benzodiazepine,5-(2-chlorophenyl)-7-fluoro-1,2-dihydro-8-methoxy-3-methyl

Pyrazolo[3,4-b][1,4]benzodiazepine, 5-(2-chlorophenyl)-7-fluoro-1,2-dihydro-8-methoxy-3-methyl-

R-1530

5-(2-Chlorophenyl)-7-fluoro-8-methoxy-3-methyl-1,2-dihydropyrazolo[3,4-b][1,4]benzodiazepine

UNII-XQJ55R5PPQ

Kinome_3737

5-(2-Chlorophenyl)-7-fluoro-1,2-dihydro-8-methoxy-3-methylpyrazolo(3,4-b)(1,4)benzodiazepine

R1530

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