ChemicalBook > CAS DataBase List > BLU9931

BLU9931

Product Name
BLU9931
CAS No.
1538604-68-0
Chemical Name
BLU9931
Synonyms
BLU;BLU9931;LM-3610;CS-1699;UBCHBEN;BLU-9931;BLU 9931;HEL-S-71;UbcH-ben;LUCA12.4
CBNumber
CB82741679
Molecular Formula
C26H22Cl2N4O3
Formula Weight
509.38
MOL File
1538604-68-0.mol
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BLU9931 Property

Density 
1.361±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
≥50.9 mg/mL in DMSO; insoluble in H2O; ≥2.53 mg/mL in EtOH with gentle warming and ultrasonic
form 
Powder
pka
13.15±0.70(Predicted)
color 
Off-white to light yellow
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H227Combustible liquid

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P210Keep away from heat/sparks/open flames/hot surfaces. — No smoking.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P370+P378In case of fire: Use … for extinction.

P403+P235Store in a well-ventilated place. Keep cool.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
18405
Product name
BLU9931
Purity
≥98%
Packaging
1mg
Price
$49
Updated
2024/03/01
Cayman Chemical
Product number
18405
Product name
BLU9931
Purity
≥98%
Packaging
5mg
Price
$216
Updated
2024/03/01
Cayman Chemical
Product number
18405
Product name
BLU9931
Purity
≥98%
Packaging
10mg
Price
$380
Updated
2024/03/01
Cayman Chemical
Product number
18405
Product name
BLU9931
Purity
≥98%
Packaging
25mg
Price
$711
Updated
2024/03/01
ChemScene
Product number
CS-4139
Product name
BLU9931
Purity
99.95%
Packaging
5mg
Price
$55
Updated
2021/12/16
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BLU9931 Chemical Properties,Usage,Production

Uses

BLU9931 is a potent, highly selective, and irreversible fibroblast growth factor receptor 4 (FGFR4) inhibitor with an IC50 of 3 nM and a Kd of 6 nM. BLU9931 has significant antitumor activity[1].

Definition

BLU9931 is a potent, highly selective, and irreversible fibroblast growth factor receptor 4 (FGFR4) inhibitor with an IC50 of 3 nM and a Kd of 6 nM. BLU9931 has significant antitumor activity. BLU9931 makes a covalent bond with Cys552 within the ATP-binding pocket of FGFR4, which is not present in FGFR1-3. BLU9931 inhibited gastric cancer cell growth in a transplanted mouse model[1].

Synthesis

1538605-10-5

814-68-6

1538604-68-0

The general procedure for the synthesis of N-[2-[[6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-quinazolinyl]amino]-3-methylphenyl]-2-acrylamide from the compound (CAS: 1538605-10-5) and acryloyl chloride was performed as follows: the N'-[6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl]- 6-methylbenzene-1,2-diamine (5.16 g, 11.33 mmol) was dissolved in dichloromethane (DCM, 100 mL) and cooled to 0 °C. Subsequently, N,N-diisopropylethylamine (DIEA, 1.781 mL, 10.20 mmol) and acryloyl chloride (1.013 mL, 12.47 mmol) were sequentially added at 0 °C and the reaction mixture was stirred for 2 h at this temperature. After completion of the reaction, the mixture was directly sampled onto a silica gel column and purified by fast column chromatography using 0-100% ethyl acetate (EtOAc)/hexane gradient elution. Finally, the target product N-[2-[[6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-quinazolinyl]amino]-3-methylphenyl]-2-propenamide was obtained as an off-white solid (3.5 g, 61% yield). The mass spectrum (electrospray positive ion mode, ES+) showed the molecular ion peak m/z 509 [M+H]+, which is consistent with the calculated value of the molecular formula C26H22Cl2N4O3.1H NMR (400 MHz, DMSO-d6) δ 9.53 (s, 1H), 9.23 (s, 1H), 8.68 (s, 1H), 7.82-7.65 (m, 2H) , 7.51 (s, 2H), 7.21 (m, 1H), 7.12 (d, J = 6.8 Hz, 1H), 7.01 (s, 1H), 6.49 (dd, J = 17.0, 10.2 Hz, 1H), 6.28-6.15 (m, 1H), 5.68 (dd, J = 10.2, 2.0 Hz, 1H), 3.97 (s, 6H) , 2.19 (s, 3H).

in vivo

BLU9931 (10-100 mg/kg; oral administration; twice every day; for 21 days; mice) treatment demonstrates antitumor activity in HCC xenograft models[1].

Animal Model:Mice injected with Hep 3B cells[1]
Dosage:10 mg/kg, 30 mg/kg or 100 mg/kg
Administration:Oral administration; twice every day; for 21 days
Result:Resulted in dose-dependent growth inhibition of Hep 3B tumors. Prevented weight loss in a dose-dependent manner.

IC 50

FGFR1: 591 nM (IC50); FGFR2: 493 nM (IC50); FGFR3: 150 nM (IC50); FGFR4: 3 nM (IC50)

References

[1] Norihiko Sasaki. “FGFR4 Inhibitor BLU9931 Attenuates Pancreatic Cancer Cell Proliferation and Invasion While Inducing Senescence: Evidence for Senolytic Therapy Potential in Pancreatic Cancer.” Cancers (2020).

BLU9931 Preparation Products And Raw materials

Raw materials

Preparation Products

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BLU9931 Suppliers

China 136 India 1 United States 11 Global 148
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6003
Advantage
61
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
sales@meilune.com
Country
China
ProdList
4747
Advantage
58
Shanghai Topbiochem Technology Co., Ltd
Tel
021-58170097
Email
info@topbiochem.com
Country
China
ProdList
9510
Advantage
58
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
Advantage
61
TargetMol Chemicals Inc.
Tel
021-021-33632979 15002134094
Fax
021-33632979
Email
marketing@targetmol.com
Country
China
ProdList
7783
Advantage
58
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3506
Advantage
58
Shanghai Synteam Biochem CO.,ltd
Tel
+86-021-58380978 13482386415
Fax
021-58380978
Email
info@systeambc.com
Country
China
ProdList
896
Advantage
50
AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Fax
025-68650336
Email
info@adooq.cn
Country
China
ProdList
2990
Advantage
60
Shanghai YuanQi Biotechnology Co., Ltd.
Tel
+86-2332782371 +86-18120098618
Email
sales@adobechem.com
Country
China
ProdList
1250
Advantage
50
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View Lastest Price from BLU9931 manufacturers

Career Henan Chemical Co
Product
BLU 9931 1538604-68-0
Price
US $1.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
10000KGS
Release date
2019-12-31

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  • BLU 9931
  • BLU9931
  • BLU-9931
  • LM-3610
  • LM-3610; BLU9931
  • 2-Propenamide,N-[2-[[6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-quinazolinyl]amino]-3-methylphenyl]-
  • BLU 9931;BLU-9931
  • BLU9931, 98%, a potent, selective, and irreversible FGFR4 inhibitor
  • N-(2-((6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl)amino)-3-methylphenyl)acrylamide
  • N-[2-[[6-(2,6-Dichloro-3,5-dimethoxyphenyl)-2-quinazolinyl]amino]-3-methylphenyl]-2-propenamide
  • BLU
  • CS-1699
  • BLU-9931;BLU 9931;BLU9931
  • BLU9931, 10 mM in DMSO
  • HEL-S-71
  • UBCHBEN
  • UbcH-ben
  • LUCA12.4
  • 1538604-68-0
  • C26H22Cl2N4O3
  • Inhibitors