ChemicalBook > CAS DataBase List > BI 882370

BI 882370

Product Name
BI 882370
CAS No.
1392429-79-6
Chemical Name
BI 882370
Synonyms
XP-102;CS-2615;BI 882370;BI882370;BI-882370;BI-882370,Raf,BI882370,inhibit,Inhibitor,Raf kinases,BI 882370;1-Propanesulfonamide, N-[3-[5-[(1-ethyl-4-piperidinyl)methylamino]-3-(5-pyrimidinyl)-1H-pyrrolo[3,2-b]pyridin-1-yl]-2,4-difluorophenyl]-;N-(3-(5-((1-Ethylpiperidin-4-yl)(methyl)amino)-3-(pyrimidin-5-yl)-1H-pyrrolo[3,2-b]pyridin-1-yl)-2,4-difluorophenyl)propane-1-sulfonamide
CBNumber
CB53358255
Molecular Formula
C28H33F2N7O2S
Formula Weight
569.67
MOL File
1392429-79-6.mol
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BI 882370 Property

Boiling point:
649.6±65.0 °C(Predicted)
Density 
1.37±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO:5.0(Max Conc. mg/mL);8.78(Max Conc. mM)
form 
A crystalline solid
pka
5.48±0.10(Predicted)
color 
Off-white to gray
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical
Product number
24273
Product name
BI-882370
Purity
≥95%
Packaging
1mg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
24273
Product name
BI-882370
Purity
≥95%
Packaging
5mg
Price
$139
Updated
2024/03/01
Cayman Chemical
Product number
24273
Product name
BI-882370
Purity
≥95%
Packaging
10mg
Price
$243
Updated
2024/03/01
Cayman Chemical
Product number
24273
Product name
BI-882370
Purity
≥95%
Packaging
25mg
Price
$533
Updated
2024/03/01
ChemScene
Product number
CS-0030522
Product name
BI-882370
Purity
99.16%
Packaging
50mg
Price
$550
Updated
2021/12/16
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BI 882370 Chemical Properties,Usage,Production

Description

BI-882370 is an orally bioavailable RAF inhibitor with IC50 values of 0.8, 0.8, and 0.6 nM for B-RAFV600E, wild-type B-RAF, and C-RAF in the DFG-out inactive conformation, respectively. It is selective for RAF over a panel of kinases, including LCK, KIT, Src, LYNA, LYNB, and PDGFR (IC50s = 49, 415, 485, 750, 715, and 1,220 nM, respectively). It inhibits proliferation of human B-RAF-mutant melanoma cells when used at concentrations ranging from 1 to 10 nM. It reduces tumor growth in multiple B-RAF-mutant melanoma and colorectal carcinoma mouse xenograft models when administered at a dose of 25 mg/kg twice per day. BI-882370, alone and in combination with trametinib , induces tumor regression in an A375 melanoma mouse xenograft model with no resistance developing within three or five weeks, respectively.

Uses

BI-882370 is a potent and selective RAF kinase inhibitor that binds to the ATP binding site of the kinase positioned in the DFG-out (inactive) conformation of the BRAF kinase. BI-882370 (BI 882370) inhibits the oncogenic BRAFV600E-mutant, the WT BRAF and CRAF kinases with IC50s of 0.4, 0.8, and 0.6 nM, respectively. BI-882370 also inhibits SRC family kinases[1].

in vivo

BI-882370 (deliver orally; 25 mg/kg, 50 mg/kg; twice daily; 2 weeks) is efficacious in multiple mouse models of BRAF-mutant melanomas and colorectal carcinomas, shows superior efficacy compared with Vemurafenib, Dabrafenib, or Trametinib[1]. BI-882370 (deliver orally; 25 mg/kg; twice daily; 40 days) developes resistance within 3 weeks, but resistance is not observed during 5 weeks of second-line therapy in combination with trametinib[1]. BI-882370 (deliver orally; 60 mg/kg; once daily; 2 weeks) indicates lack of toxicity in terms of clinical chemistry, hematology, pathology, and toxicogenomics in rats[1].

Animal Model:Human melanoma xenografts in nude mice with BRAF-mutant melanomas and colorectal carcinomas cells (A375, COLO 205; G-361, HT-29 cells)[1]
Dosage:25 mg/kg; 50 mg/kg
Administration:Deliver orally; 25 mg/kg, 50 mg/kg; twice daily; 2 weeks
Result:Regressed tumors partially, upon discontinuation, tumor regrowth was markedly delayed.

IC 50

Braf: 0.6 nM (IC50); c-Raf: 0.8 nM (IC50); BRafV600E: 0.4 nM (IC50)

References

[1] Waizenegger IC, et al. A Novel RAF Kinase Inhibitor with DFG-Out-Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation. Mol Cancer Ther. 2016 Mar;15(3):354-65. DOI:10.1158/1535-7163.MCT-15-0617

BI 882370 Preparation Products And Raw materials

Raw materials

Preparation Products

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BI 882370 Suppliers

China 52 United States 7 Global 59
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
BOC Sciences
Tel
1-631-485-4226; 16314854226
Email
info@bocsci.com
Country
United States
ProdList
12952
Advantage
65
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4768
Advantage
55
BOC Sciences
Tel
16314854226
Email
info@bocsci.com
Country
United States
ProdList
9923
Advantage
65
Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Fax
021-65675885
Email
info@efebio.com
Country
China
ProdList
9803
Advantage
58
ShangHai Biochempartner Co.,Ltd
Tel
177-54423994 17754423994
Fax
QQ:2853530913
Email
2853530910@QQ.com
Country
China
ProdList
8000
Advantage
62
Chuzhou KeMail Chemical Technology Co., Ltd
Tel
0550-5196001 15000891977
Fax
0550-5196001
Email
wj520wjxby@126.com
Country
China
ProdList
1944
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Shanghai Biopharmaleader Co., Ltd.
Tel
+86 18721201413
Fax
+86 (21) 5775-8967
Email
sales@biopharmaleader.com
Country
China
ProdList
1720
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58
Twochem Co.Ltd.
Tel
021-58111628 15800915896
Fax
QQ 3285589261
Email
sales@twochem.com
Country
China
ProdList
1788
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58
Jinan Yaoyan Pharmaceutical Co., Ltd.
Tel
Fax
-
Email
jnyaoyan@163.com
Country
China
ProdList
3069
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58

1392429-79-6, BI 882370Related Search:


  • BI 882370
  • BI882370;BI-882370
  • 1-Propanesulfonamide, N-[3-[5-[(1-ethyl-4-piperidinyl)methylamino]-3-(5-pyrimidinyl)-1H-pyrrolo[3,2-b]pyridin-1-yl]-2,4-difluorophenyl]-
  • CS-2615
  • BI-882370,Raf,BI882370,inhibit,Inhibitor,Raf kinases,BI 882370
  • N-(3-(5-((1-Ethylpiperidin-4-yl)(methyl)amino)-3-(pyrimidin-5-yl)-1H-pyrrolo[3,2-b]pyridin-1-yl)-2,4-difluorophenyl)propane-1-sulfonamide
  • XP-102
  • 1392429-79-6
  • C28H33F2N7O2S
  • BI 882370