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Tocris/BIBX 1382 dihydrochloride/2416/10/10 mg

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货号: 2416/10

品牌: Tocris

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Description: Highly selective EGFR-kinase inhibitor

Chemical Name: N⁸-(3-Chloro-4-fluorophenyl)-N²-(1-methyl-4-piperidinyl)-pyrimido[5,4-d]pyrimidine-2,8-diamine dihydrochloride

Purity: ≥97% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Potent, selective inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase (IC₅₀ = 3 nM). Displays > 1000-fold lower potency against ErbB2 (IC₅₀ = 3.4 μM) and a range of other related tyrosine kinases (IC₅₀ > 10 μM). Oral administration inhibits growth of established human xenografts in athymic mice.

Compound Libraries

BIBX 1382 dihydrochloride is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	460.77
Formula	C₁₈H₁₉ClFN₇.2HCl
Storage	Desiccate at +4°C
Purity	≥97% (HPLC)
CAS Number	1216920-18-1
PubChem ID	46861540
InChI Key	RFXGEKWBTCMDAW-UHFFFAOYSA-N
Smiles	Cl.Cl.CN1CCC(CC1)NC1=NC=C2N=CN=C(NC3=CC(Cl)=C(F)C=C3)C2=N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	19.39	50
	water	19.39	50

Preparing Stock Solutions

The following data is based on the product molecular weight 460.77. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.17 mL	10.85 mL	21.7 mL
5 mM	0.43 mL	2.17 mL	4.34 mL
10 mM	0.22 mL	1.09 mL	2.17 mL
50 mM	0.04 mL	0.22 mL	0.43 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Dittrich et al (2002) Phase I and pharmacokinetic study of BIBX1382 BS, an epidermal growth factor receptor (EGFR) inhibitor, given in a continuous daily oral administration. Eur.J.Cancer 38 1072 PMID: 12008195

Solca et al (2004) Inhibition of epidermal growth factor receptor activity by two pyrimidopyrimidine derivatives. J.Pharmacol.Exp.Ther. 311 502 PMID: 15199094

Keywords: BIBX 1382 dihydrochloride, supplier, selective, EGFR-kinases, inhibitors, inhibits, Epidermal, Growth, Factors, Receptors, ErbB, Her, Receptor, Tyrosine, Kinases, RTKs, BIBX1382, dihydrochloride, EGFR, EGFR, Tocris Bioscience

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