Basic information Safety Supplier Related

BIBX 1382 DIHYDROCHLORIDE

Basic information Safety Supplier Related

BIBX 1382 DIHYDROCHLORIDE Basic information

Product Name:
BIBX 1382 DIHYDROCHLORIDE
Synonyms:
  • FALNIDAMOL; BIBX-1382; BIBX 1382
  • BIBX 1382 dihydrochloride,N8-(3-Chloro-4-fluorophenyl)-N2-(1-methyl-4-piperidinyl)-pyrimido[5,4-d]pyrimidine-2,8-diaminedihydrochloride
  • CS-928
  • BIBX 1382 DIHYDROCHLORIDE
  • 8-(3-Chloro-4-fluoroanilino)-2-((1-methyl-4-piperidyl)amino)pyrimido(5,4-D)pyrimidine
  • Falnidamol
  • Falnidamol [inn]
  • Pyrimido(5,4-D)pyrimidine-2,8-diamine, N8-(3-chloro-4-fluorophenyl)-N2-(1-methyl-4-piperidinyl)-
CAS:
196612-93-8
MF:
C18H19ClFN7
MW:
387.84
Mol File:
196612-93-8.mol
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BIBX 1382 DIHYDROCHLORIDE Chemical Properties

Melting point:
>217°C (dec.)
Boiling point:
552.0±60.0 °C(Predicted)
Density 
1.427
storage temp. 
Keep in dark place,Inert atmosphere,2-8°C
solubility 
DMSO (Slightly), Methanol (Slightly)
pka
8?+-.0.10(Predicted)
form 
Solid
color 
Pale Yellow to Yellow
Water Solubility 
water: 1mg/mL
DMSO: 25mg/mL
InChI
1S/C18H19ClFN7/c1-27-6-4-11(5-7-27)25-18-21-9-15-16(26-18)17(23-10-22-15)24-12-2-3-14(20)13(19)8-12/h2-3,8-11H,4-7H2,1H3,(H,21,25,26)(H,22,23,24)
InChIKey
FTFRZXFNZVCRSK-UHFFFAOYSA-N
SMILES
Fc1c(cc(cc1)Nc2ncnc3c2nc(nc3)NC4CCN(CC4)C)Cl
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Safety Information

WGK Germany 
WGK 2
Storage Class
11 - Combustible Solids
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BIBX 1382 DIHYDROCHLORIDE Usage And Synthesis

Uses

Falnidamol is a novel ErbB receptor kinase inhibitor that is more potent at inhibiting signaling induced by TGF-α than that induced by neuregulin1-β1 or anti-ErbB2 agonist antibodies.

Uses

BIBX 1382 Dihydrochloride, is a potent, selective inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase (IC50 = 3 nM).

Definition

ChEBI: N4-(3-chloro-4-fluorophenyl)-N6-(1-methyl-4-piperidinyl)pyrimido[5,4-d]pyrimidine-4,6-diamine is a substituted aniline.

Biological Activity

Potent, selective inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase (IC 50 = 3 nM). Displays > 1000-fold lower potency against ErbB2 (IC 50 = 3.4 μ M) and a range of other related tyrosine kinases (IC 50 > 10 μ M). Oral administration inhibits growth of established human xenografts in athymic mice.

in vivo

Falnidamol (BIBX 1382; p.o.; 10 mg/kg/day; 16 days) completely suppressed tumor growth of human A431 xenografts with respective a T/C value of 15% after 2 weeks of treatment[2].
Falnidamol (50 mg/kg/day for 2 weeks) results in dephosphorylation of the EGF receptor in A431 xenograft-bearing mice[2].
With Falnidamol (p.o.; 10 mg/kg/day; 16 days), the C4h is 2222 nM and the C24h is 244 nM[2].

Animal Model:Five- to six-week-old athymic NMRI-nu/nu female mice (21-31 g) with A431, FaDu, or HN5 cells[2]
Dosage:10 mg/kg
Administration:p.o.; daily; 16 days
Result:Completely suppressed tumor growth of human A431 xenografts with respective T/C values of 15 and 6% after 2 weeks of treatment.
Animal Model:Five- to six-week-old athymic NMRI-nu/nu female mice (21–31 g) with A431 cells[2]
Dosage:10 mg/kg (Pharmacokinetic Analysis)
Administration:p.o.; daily; 16 days
Result:The C4h is 2222 nM and the C24h is 244 nM.

IC 50

EGFR: 3 nM (IC50); ErbB2: 3.4 μM (IC50)

References

1. f. f. solca, a. baum, e. langkopf, g. dahmann, k. h. heider, f. himmelsbach and j. c. van meel, j pharmacol exp ther 2004, 311, 502-509.

BIBX 1382 DIHYDROCHLORIDESupplier

Shanghai Boyle Chemical Co., Ltd.
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Email
sales@boylechem.com
3B Pharmachem (Wuhan) International Co.,Ltd.
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821-50328103-801 18930552037
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3bsc@sina.com
Chembest Research Laboratories Limited
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+86-21-20908456
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sales@BioChemBest.com
Beijing HuaMeiHuLiBiological Chemical
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010-56205725
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waley188@sohu.com
Haoyuan Chemexpress Co., Ltd.
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021-58950125
Email
info@chemexpress.com
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