ChemicalBook >> CAS DataBase List >>6-(4-Methyl-1-piperazinyl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(1E)-2-phenylethenyl]-4-pyrimidinamine

6-(4-Methyl-1-piperazinyl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(1E)-2-phenylethenyl]-4-pyrimidinamine

6-(4-Methyl-1-piperazinyl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(1E)-2-phenylethenyl]-4-pyrimidinamine structure

CAS No.: 934353-76-1

Chemical Name:: 6-(4-Methyl-1-piperazinyl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(1E)-2-phenylethenyl]-4-pyrimidinamine

Synonyms: ENMD-2076;CS-406;ENMD2076, >98%;ENMD-2076, >98%;(E)-N-(5-methyl-1H-pyrazol-3-yl)-6-(4-methylpiperazin-1-yl)-2-styrylpyrimidin-4-amine;6-(4-methylpiperazin-1-yl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(E)-2-phenylethenyl]pyrimidin-4-amine;6-(4-Methyl-1-piperazinyl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(1E)-2-phenylethenyl]-4-pyrimidinamine;4-Pyrimidinamine, 6-(4-methyl-1-piperazinyl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(1E)-2-phenylethenyl]-;6-(4-Methyl-1-piperazinyl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(1E)-2-phenylethenyl]-4-pyrimidinamine USP/EP/BP;6-(4-Methyl-1-piperazinyl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(1E)-2-phenylethenyl]-4-pyrimidinamine ENMD-2076

CBNumber:: CB12509979

Molecular Formula:: C21H25N7

Molecular Weight:: 375.47

MDL Number:: MFCD16619371

MOL File:: 934353-76-1.mol

Last updated:2023-09-28 17:55:30

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6-(4-Methyl-1-piperazinyl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(1E)-2-phenylethenyl]-4-pyrimidinamine Properties

Density	1.267
storage temp.	Store at -20°C
solubility	insoluble in H2O; ≥18.75 mg/mL in DMSO; ≥2.55 mg/mL in EtOH with ultrasonic
form	solid
CAS DataBase Reference	934353-76-1
FDA UNII	J6U9WP10T7

SAFETY

Risk and Safety Statements

Symbol(GHS)	GHS07
Signal word	Warning
Hazard statements	H302-H315-H319-H335
Precautionary statements	P261-P305+P351+P338

6-(4-Methyl-1-piperazinyl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(1E)-2-phenylethenyl]-4-pyrimidinamine price More Price(22)

Manufacturer	Product number	Product description	CAS number	Packaging	Price	Updated	Buy
Cayman Chemical	22956	ENMD-2076 ≥98%	934353-76-1	1mg	$40	2021-12-16	Buy
Cayman Chemical	22956	ENMD-2076 ≥98%	934353-76-1	5mg	$160	2021-12-16	Buy
Cayman Chemical	22956	ENMD-2076 ≥98%	934353-76-1	10mg	$300	2021-12-16	Buy
ApexBio Technology	A4130	ENMD-2076	934353-76-1	50mg	$400	2021-12-16	Buy
ChemScene	CS-0836	ENMD-2076 99.12%	934353-76-1	50mg	$540	2021-12-16	Buy

Product number	Packaging	Price	Buy
22956	1mg	$40	Buy
22956	5mg	$160	Buy
22956	10mg	$300	Buy
A4130	50mg	$400	Buy
CS-0836	50mg	$540	Buy

6-(4-Methyl-1-piperazinyl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(1E)-2-phenylethenyl]-4-pyrimidinamine Chemical Properties,Uses,Production

Description

ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. Phase 2.

Features

Multi-target, anti-proliferative, pro-apoptotic activity, anti-angiogenic.

In vitro

ENMD-2076 indicates activity against multiple kinases involved in angiogenesis, including FLT3, RET, FLT4/VEGFR3, SRC, NTRK1, CSF1R/FMS, LCK, VEGFR2/KDR, FGFR1/2, and PDGFRα with IC50 from 1.86-120 nM. ENMD-2076 inhibits the growth of a wide range of human solid tumor and hematopoietic cancer cell lines with IC50 from 0.025 to 0.7 μM, which induces apoptosis and G2/M phase arrest. ENMD-2076 induces regression or complete inhibition of tumor growth in tumor xenograft models derived from breast, colon, melanoma, leukemia, and multiple myeloma cell lines. ENMD-2076 is the L (+) tartrate salt of ENMD-981693. ENMD-2076 shows significant cytotoxicity against myeloma cell lines (IM9, ARH-77, U266, RPMI 8226, MM.1S, MM.1R, NCI-H929) and primary cells with IC50 from 2.99 to 7.06 μM, which induces apoptosis. ENMD-2076 indicates low cytotoxicity to haematopoietic progenitors. ENMD-2076 inhibits the phosphoinositide 3-kinase/Akt pathway and downregulates survivin and X-linked inhibitor of apoptosis. ENMD-2076 also inhibits aurora A and B kinases, and induces G2/M cell cycle arrest.

In vivo

ENMD-2076 has sustained inhibitory effects on the activation of Flt3 as well as VEGFR2/KDR and FGFR1/2 in HT29 xenograft model. ENMD-2076 could prevent the formation of new blood vessels and regress formed vessels in MDA-MB-231 xenograft model. Oral treatment with ENMD-2076 (50, 100, 200 mg/kg per day) inhibits the tumour growth in H929 human plasmacytoma xenografts, with significant reduction in phospho-Histone 3 (pH3), Ki-67, and angiogenesis, and also a significant increase in cleaved caspase-3.

Biological Activity

enmd-2076 is a selective inhibitor of aurora a and flt3 with ic50 value of 14 and 1.86 nm[1].aurora kinases contains aurora a, aurora b and aurora c. they are serine/threonine kinases witch play an important role in cell proliferation. aurora kinases are essential for cellular division by controlling segregation of chromatid. aurora a is required for correct function of the centrosomes during the prophase of mitosis [1]. vegfr (vegf receptors) are receptors for vegf (vascular endothelial growth factor). there are vegfr 1, 2 and 3 which three main subtypes of vegfr. the vegfrs are tyrosine kinase receptors which are activited by binding to vegfs then mediate the cellular responses to vegf including the formation of the circulatory system (vasculogenesis) and the growth of blood vessels(angiogenesis) [1].enmd-2076 indicates activities of ret, flt3, flt4/vegfr3, src, csf1r/fms, ntrk1, fgfr1/2, vegfr2/kdr, lck, and pdgfrα which all are kinases involved in angiogenes with ic50 from 1.86-120 nm. enmd-2076 can inhibit the growth of hematopoietic cancer cell lines and lots of solid tumor with ic50 values from 25 to 700 nm in vitro[1]. enmd-2076 significantly caused cytotoxicity in multiple myeloma (mm) cell lines and primary cells. enmd-2076 also inhibited the phosphoinositide 3-kinase (pi3k)/akt pathway. enmd-2076 also induced cell cycle arrest in g2/m phase by inhibiting the activities of aurora kinases containing a and b class.[2]enmd-2076 regresses formed vessels and prevents new blood vessels formation in tumorxenograft models. [1] enmd-2076 resulted in inhibition of tumour growth with oral treatment a dose-dependent manner with 50, 100, 200 mg/kg per day with human plasmacytoma xenografts[2].

target

Aurora A

References

[1]. fletcher gc, brokx rd, denny ta, hembrough ta, plum sm, fogler we, sidor cf, bray mr: enmd-2076 is an orally active kinase inhibitor with antiangiogenic and antiproliferative mechanisms of action. mol cancer ther 2011, 10(1):126-137.
[2]. wang x, sinn al, pollok k, sandusky g, zhang s, chen l, liang j, crean cd, suvannasankha a, abonour r et al: preclinical activity of a novel multiple tyrosine kinase and aurora kinase inhibitor, enmd-2076, against multiple myeloma. br j haematol 2010, 150(3):313-325.

6-(4-Methyl-1-piperazinyl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(1E)-2-phenylethenyl]-4-pyrimidinamine Preparation Products And Raw materials

Raw materials

Preparation Products

6-(4-Methyl-1-piperazinyl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(1E)-2-phenylethenyl]-4-pyrimidinamine Suppliers

Global( 93)Suppliers

Supplier	Tel	Email	Country	ProdList	Advantage
Hebei Mojin Biotechnology Co., Ltd	+8613288715578	sales@hbmojin.com	China	12456	58
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32480	60
career henan chemical co	+86-0371-86658258	sales@coreychem.com	China	29914	58
Hubei xin bonus chemical co. LTD	86-13657291602	linda@hubeijusheng.com	CHINA	22968	58
BOC Sciences	+1-631-485-4226	inquiry@bocsci.com	United States	19553	58
Chongqing Chemdad Co., Ltd	+86-023-61398051 +8613650506873	sales@chemdad.com	China	39916	58
CONIER CHEM AND PHARMA LIMITED	+8618523575427	sales@conier.com	China	49390	58
TargetMol Chemicals Inc.	+1-781-999-5354 +1-00000000000	marketing@targetmol.com	United States	19892	58
Dideu Industries Group Limited	+86-29-89586680 +86-15129568250	1026@dideu.com	China	29220	58
Hefei Hirisun Pharmatech Co., Ltd	+8615056975894	shawn@hirisunpharm.com	CHINA	9923	58

Supplier	Advantage
Hebei Mojin Biotechnology Co., Ltd	58
ATK CHEMICAL COMPANY LIMITED	60
career henan chemical co	58
Hubei xin bonus chemical co. LTD	58
BOC Sciences	58
Chongqing Chemdad Co., Ltd	58
CONIER CHEM AND PHARMA LIMITED	58
TargetMol Chemicals Inc.	58
Dideu Industries Group Limited	58
Hefei Hirisun Pharmatech Co., Ltd	58

View Lastest Price from 6-(4-Methyl-1-piperazinyl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(1E)-2-phenylethenyl]-4-pyrimidinamine manufacturers

Image	Update time	Product	Price	Min. Order	Purity	Supply Ability	Manufacturer
	2023-09-28	6-(4-Methyl-1-piperazinyl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(1E)-2-phenylethenyl]-4-pyrimidinamine 934353-76-1	US $0.00 / KG	1KG	99%	5000	Hebei Mojin Biotechnology Co., Ltd
	2019-07-06	6-(4-Methyl-1-piperazinyl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(1E)-2-phenylethenyl]-4-pyrimidinamine 934353-76-1	US $2.00 / kg	1kg	99%	100kg	Career Henan Chemical Co

6-(4-Methyl-1-piperazinyl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(1E)-2-phenylethenyl]-4-pyrimidinamine
934353-76-1
US $0.00 / KG
99%
Hebei Mojin Biotechnology Co., Ltd

6-(4-Methyl-1-piperazinyl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(1E)-2-phenylethenyl]-4-pyrimidinamine
934353-76-1
US $2.00 / kg
99%
Career Henan Chemical Co

6-(4-Methyl-1-piperazinyl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(1E)-2-phenylethenyl]-4-pyrimidinamine Spectrum

6-(4-Methyl-1-piperazinyl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(1E)-2-phenylethenyl]-4-pyrimidinamine(934353-76-1)¹HNMR

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1of3

6-(4-Methyl-1-piperazinyl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(1E)-2-phenylethenyl]-4-pyrimidinamine (E)-N-(5-methyl-1H-pyrazol-3-yl)-6-(4-methylpiperazin-1-yl)-2-styrylpyrimidin-4-amine 6-(4-Methyl-1-piperazinyl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(1E)-2-phenylethenyl]-4-pyrimidinamine ENMD-2076 ENMD2076, >98% ENMD-2076, >98% CS-406 4-Pyrimidinamine, 6-(4-methyl-1-piperazinyl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(1E)-2-phenylethenyl]- 6-(4-Methyl-1-piperazinyl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(1E)-2-phenylethenyl]-4-pyrimidinamine USP/EP/BP 6-(4-methylpiperazin-1-yl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(E)-2-phenylethenyl]pyrimidin-4-amine ENMD-2076 934353-76-1 Inhibitors Inhibitor