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BIBX 1382 DIHYDROCHLORIDE

Product Name
BIBX 1382 DIHYDROCHLORIDE
CAS No.
196612-93-8
Chemical Name
BIBX 1382 DIHYDROCHLORIDE
Synonyms
Falnid;CS-928;Falnidamol;Unii-0mu316797d;Falnidamol [inn];BIBX 1382 DIHYDROCHLORIDE;Falnidamol, 10 mM in DMSO;EGFR Inhibitor II, BIBX1382;FALNIDAMOL; BIBX-1382; BIBX 1382;8-(3-Chloro-4-fluoroanilino)-2-((1-methyl-4-piperidyl)amino)pyrimido(5,4-D)pyrimidine
CBNumber
CB6842590
Molecular Formula
C18H19ClFN7
Formula Weight
387.84
MOL File
196612-93-8.mol
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BIBX 1382 DIHYDROCHLORIDE Property

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
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

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

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
324832
Product name
EGFR Inhibitor II, BIBX1382 - CAS 196612-93-8 - Calbiochem
Packaging
5MG
Price
$318
Updated
2024/03/01
Cayman Chemical
Product number
29630
Product name
BIBX1382
Packaging
1mg
Price
$34
Updated
2024/03/01
Cayman Chemical
Product number
29630
Product name
BIBX1382
Packaging
25mg
Price
$576
Updated
2024/03/01
Cayman Chemical
Product number
29630
Product name
BIBX1382
Packaging
5mg
Price
$150
Updated
2024/03/01
Cayman Chemical
Product number
29630
Product name
BIBX1382
Packaging
10mg
Price
$280
Updated
2024/03/01
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BIBX 1382 DIHYDROCHLORIDE Chemical Properties,Usage,Production

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 DIHYDROCHLORIDE Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from BIBX 1382 DIHYDROCHLORIDE manufacturers

Career Henan Chemical Co
Product
BIBX 1382 dihydrochloride,N8-(3-Chloro-4-fluorophenyl)-N2-(1-methyl-4-piperidinyl)-pyrimido[5,4-d]pyrimidine-2,8-diaminedihydrochloride 196612-93-8
Price
US $1.00/KG
Min. Order
1KG
Purity
Min98% HPLC
Supply Ability
g/kg/ton
Release date
2019-12-30

196612-93-8, BIBX 1382 DIHYDROCHLORIDERelated Search:

Piperidin-4-yl-pyrimidin-2-yl-amine dihydrochloride BIBX 1382 DIHYDROCHLORIDE

  • 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)-
  • Unii-0mu316797d
  • N8-(3-Chloro-4-fluorophenyl)-N2-(1-methyl-4-piperidinyl)-pyrimido[5,4-d]pyrimidine-2,8-diaminedihydrochloride
  • Falnid
  • N8-(3-Chloro-4-fluorophenyl)-N2-(1-methyl-4-piperidinyl)pyrimido[5,4-d]pyrimidine-2,8-diamine
  • N8-(3-Chloro-4-fluorophenyl)-N2-(1-methyl-4-piperidinyl)pyrimido[5,4-d]pyrimidine-2,8-diamine BIBX 1382
  • N8-(3-Chloro-4-fluorophenyl)-N2-(1-methylpiperidin-4-yl)pyrimido[5,4-d]pyrimidine-2,8-diamine
  • N4-(3-chloro-4-fluoro-phenyl)-N6-(1-methyl-4-piperidyl)pyrimido[5,4-d]pyrimidine-4,6-diamine
  • N8-(3-CHLORO-4-FLUOROPHENYL)-N2-(1-METHYL-4-PIPERIDINYL)-PYRIMIDO[5,4-D]PYRIMIDINE-2,8-DIAMINE DIHYDROCHLORIDE
  • Falnidamol, 10 mM in DMSO
  • EGFR Inhibitor II, BIBX1382
  • 196612-93-8
  • C18H19ClFN7
  • C18H21Cl3FN7
  • C18H19ClFN72HCl