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H3B-6527

H3B-6527 structure

CAS No.: 1702259-66-2

Chemical Name:: H3B-6527

Synonyms: CS-2347;H3B-6527;H3 Biomedicine;H3B6527;H3B 6527;Eisai/H3 Biomedicine;H-3B-6527,H3B6527,H3B 6527;H3B-6527, 98%, a highly selective FGFR4 inhibitor with potent antitumour activity;N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-yl)phenyl)acrylamide;2-Propenamide, N-[2-[[6-[[[(2,6-dichloro-3,5-dimethoxyphenyl)amino]carbonyl]methylamino]-4-pyrimidinyl]amino]-5-(4-ethyl-1-piperazinyl)phenyl]-

CBNumber:: CB23146613

Molecular Formula:: C29H34Cl2N8O4

Molecular Weight:: 629.54

MDL Number:: MFCD30377210

MOL File:: 1702259-66-2.mol

Last updated:2023-05-21 10:59:17

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H3B-6527 Properties

Boiling point	832.1±65.0 °C(Predicted)
Density	1.373±0.06 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMSO:50.0(Max Conc. mg/mL);79.42(Max Conc. mM)
form	A solid
pka	11.00±0.70(Predicted)
FDA UNII	4HTE364XIK

H3B-6527 price More Price(13)

Manufacturer	Product number	Product description	CAS number	Packaging	Price	Updated	Buy
Cayman Chemical	26072	H3B-6527 ≥98%	1702259-66-2	1mg	$81	2024-03-01	Buy
Cayman Chemical	26072	H3B-6527 ≥98%	1702259-66-2	5mg	$238	2024-03-01	Buy
Cayman Chemical	26072	H3B-6527 ≥98%	1702259-66-2	10mg	$435	2024-03-01	Buy
Cayman Chemical	26072	H3B-6527 ≥98%	1702259-66-2	25mg	$887	2024-03-01	Buy
AK Scientific	2308EF	H3B-6527	1702259-66-2	1mg	$187	2021-12-16	Buy

Product number	Packaging	Price	Buy
26072	1mg	$81	Buy
26072	5mg	$238	Buy
26072	10mg	$435	Buy
26072	25mg	$887	Buy
2308EF	1mg	$187	Buy

H3B-6527 Chemical Properties,Uses,Production

Biological Activity

H3B-6527 is a highly selective covalent FGFR4 inhibitor with IC50 < 1.2 nM, with >250-fold selectivity for FGFR4 over FGFR1-3 (IC50s of 320, 1290 and 1290 for FGFR1-3, respectively) 1060 nM).

in vitro

H3B-6527 has a strong inhibitory effect on FGFR4 with IC50 less than 1.2 nM. TAOK2, JNK2 and CSF1R were less sensitive to H3B-6527 treatment with IC50s of 690, >10000 and >10000 nmol/L, respectively. Treatment of Hep3B cells with H3B-6527 resulted in a concentration-dependent activation of caspase-3/7. It inhibits FGFR4 signaling, inhibits proliferation, and causes apoptosis in HCC cells.

in vivo

In a mouse model of Hep3B hepatocarcinoma xenografts, H3B-6527 had dose-proportional plasma exposure (greater than tumor exposure; doses tested were 30, 100, and 300 mg/kg). The pharmacodynamic response of H3B-6527 was detected, and it was found that CYP7A1 mRNA and pERK1/2 protein levels showed a concentration-dependent response, and higher concentrations would lead to a more durable response. In both subcutaneous Hep3B xenograft models and orthotopic xenograft models, oral administration of it (twice a day) significantly inhibited the growth of xenografts. Palbociclib enhanced the potency of it and promoted tumor regression in the JHH-7 model, whereas it single-agent administration only caused tumor growth arrest.

H3B-6527 Preparation Products And Raw materials

Raw materials

Preparation Products

H3B-6527 Suppliers

Global( 66)Suppliers

Supplier	Tel	Email	Country	ProdList	Advantage
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32480	60
BOC Sciences	+1-631-485-4226	inquiry@bocsci.com	United States	19553	58
Neostar United (Changzhou) Industrial Co., Ltd.	+86-519-519-85557386	marketing1@neostarunited.com	China	8349	58
HANGZHOU CLAP TECHNOLOGY CO.,LTD	86-571-88216897,88216896 13588875226	sales@hzclap.com	CHINA	6313	58
AFINE CHEMICALS LIMITED	0571-85134551	info@afinechem.com	CHINA	15377	58
Finetech Industry Limited	+86-27-87465837 +8618971612321	info@finetechnology-ind.com	China	9702	58
Zhejiang J&C Biological Technology Co.,Limited	+1-2135480471 +1-2135480471	sales@sarms4muscle.com	China	10523	58
InvivoChem	+1-708-310-1919 +1-13798911105	sales@invivochem.cn	United States	6393	58
Nantong HI-FUTURE Biology Co., Ltd.	+undefined18051384581	sales@chemhifuture.com	China	3136	58
TargetMol Chemicals Inc.	+1-781-999-5354	support@targetmol.com	United States	19973	58

Supplier	Advantage
ATK CHEMICAL COMPANY LIMITED	60
BOC Sciences	58
Neostar United (Changzhou) Industrial Co., Ltd.	58
HANGZHOU CLAP TECHNOLOGY CO.,LTD	58
AFINE CHEMICALS LIMITED	58
Finetech Industry Limited	58
Zhejiang J&C Biological Technology Co.,Limited	58
InvivoChem	58
Nantong HI-FUTURE Biology Co., Ltd.	58
TargetMol Chemicals Inc.	58

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H3B-6527 N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-yl)phenyl)acrylamide Eisai/H3 Biomedicine H3B-6527, 98%, a highly selective FGFR4 inhibitor with potent antitumour activity CS-2347 H3B6527;H3B 6527 2-Propenamide, N-[2-[[6-[[[(2,6-dichloro-3,5-dimethoxyphenyl)amino]carbonyl]methylamino]-4-pyrimidinyl]amino]-5-(4-ethyl-1-piperazinyl)phenyl]- H-3B-6527,H3B6527,H3B 6527 H3 Biomedicine 1702259-66-2 C29H34Cl2N8O4