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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;H3B-6527, 10 mM in DMSO;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:2025-04-18 09:51:53

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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)
color	White to khaki
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

Uses

H3B-6527 is an orally active, highly selective and covalent FGFR4 inhibitor with an IC50 of <1.2 nM. H3B-6527 has at least 250-fold selectivity over FGFR1-3 with IC50s of 320 nM, 1290 nM and 1060 nM respectively. H3B-6527 has potent anti-cancer activity[1].

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.

IC 50

FGFR4: <1.2 nM (IC₅₀); FGFR1: 320 nM (IC₅₀); FGFR2: 1290 nM (IC₅₀); FGFR3: 1060 nM (IC₅₀)

References

[1] Joshi JJ, et al. H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven HepatocellularCarcinoma. Cancer Res. 2017 Dec 15;77(24):6999-7013. DOI:10.1158/0008-5472.CAN-17-1865

H3B-6527 Preparation Products And Raw materials

Raw materials

Preparation Products

H3B-6527 Suppliers

Global( 81)Suppliers

Supplier	Tel	Email	Country	ProdList	Advantage
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	33024	60
BOC Sciences	+1-631-485-4226	inquiry@bocsci.com	United States	19552	58
HANGZHOU CLAP TECHNOLOGY CO.,LTD	86-571-88216897,88216896 13588875226	sales@hzclap.com	CHINA	6312	58
AFINE CHEMICALS LIMITED	+86-0571-85134551	sales@afinechem.com	China	15417	58
Finetech Industry Limited	+86-27-8746-5837 +8619945049750	info@finetechnology-ind.com	China	9642	58
Zhejiang J&C Biological Technology Co.,Limited	+1-2135480471 +1-2135480471	sales@sarms4muscle.com	China	10473	58
InvivoChem	+1-708-310-1919 +1-13798911105	sales@invivochem.cn	United States	6391	58
Nantong HI-FUTURE Biology Co., Ltd.	+undefined18051384581	sales@chemhifuture.com	China	3135	58
TargetMol Chemicals Inc.		support@targetmol.com	United States	38663	58
Wuhan Topule Biopharmaceutical Co., Ltd	+8618327326525	masar@topule.com	China	8467	58

Supplier	Advantage
ATK CHEMICAL COMPANY LIMITED	60
BOC Sciences	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
Wuhan Topule Biopharmaceutical Co., Ltd	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 H3B-6527, 10 mM in DMSO 1702259-66-2 C29H34Cl2N8O4