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BIBU 1361 dihydrochloride

EGFR inhibitor CAS# 793726-84-8

BIBU 1361 dihydrochloride

Catalog No. BCC7356----Order now to get a substantial discount!

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BIBU 1361 dihydrochloride: 5mg $656 In Stock
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Chemical structure

BIBU 1361 dihydrochloride

3D structure

Chemical Properties of BIBU 1361 dihydrochloride

Cas No. 793726-84-8 SDF Download SDF
PubChem ID 46861539 Appearance Powder
Formula C22H29Cl3FN7 M.Wt 516.87
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in water and to 25 mM in DMSO
Chemical Name N-(3-chloro-4-fluorophenyl)-6-[4-(diethylaminomethyl)piperidin-1-yl]pyrimido[5,4-d]pyrimidin-4-amine;dihydrochloride
SMILES CCN(CC)CC1CCN(CC1)C2=NC=C3C(=N2)C(=NC=N3)NC4=CC(=C(C=C4)F)Cl.Cl.Cl
Standard InChIKey ZNNWCQCQUKAMGL-UHFFFAOYSA-N
Standard InChI InChI=1S/C22H27ClFN7.2ClH/c1-3-30(4-2)13-15-7-9-31(10-8-15)22-25-12-19-20(29-22)21(27-14-26-19)28-16-5-6-18(24)17(23)11-16;;/h5-6,11-12,14-15H,3-4,7-10,13H2,1-2H3,(H,26,27,28);2*1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of BIBU 1361 dihydrochloride

DescriptionPotent inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase (IC50 = 3 nM). Displays ~ 100-fold lower potency against ErbB2 (IC50 = 290 nM) and is selective over a range of other related tyrosine kinases (IC50 > 10 μM). Blocks downstream EGFR signaling events such as MAPKK/MAPK activation. Oral administration inhibits growth of established human xenografts in athymic mice.

BIBU 1361 dihydrochloride Dilution Calculator

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BIBU 1361 dihydrochloride Molarity Calculator

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Preparing Stock Solutions of BIBU 1361 dihydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.9347 mL 9.6736 mL 19.3472 mL 38.6944 mL 48.3681 mL
5 mM 0.3869 mL 1.9347 mL 3.8694 mL 7.7389 mL 9.6736 mL
10 mM 0.1935 mL 0.9674 mL 1.9347 mL 3.8694 mL 4.8368 mL
50 mM 0.0387 mL 0.1935 mL 0.3869 mL 0.7739 mL 0.9674 mL
100 mM 0.0193 mL 0.0967 mL 0.1935 mL 0.3869 mL 0.4837 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on BIBU 1361 dihydrochloride

BIBU 1361 dihydrochloride is a selective inhibitor of epidermal growth factor receptor (EGFR) kinase with an IC50 value of 0.038 ± 0.007 μM [1, 2].

The EGFR signaling pathway is associated with multiple intracellular signaling events that promote proliferation and survival. It plays a key role in the progression of glioblastoma multiforme (GBM) [2].

In glioma cells, EGFR signaling can induce the phosphorylation of Akt, Erk1/2 and STAT3. BIBU 1361 decreased levels of EGFR and subsequently decreased levels of p-EGFR. This effect was accompanied by the decrease in pAkt and the downstream target p-mTOR. P-S6 kinase and p-P70S6 kinase are two key targets of p-mTOR. Both of them are associated with cell proliferation. In glioma cells treated with BIBU 1361, P-S6 kinase and p-P70S6 kinase were also downregulated. E2F1 is a G1/S regulator. E2F1 is known to be interacted with by EGFR. The inhibition of Akt/mTOR signaling can affect cell cycle progression. In glioma cells, BIBU 1361 inhibited the expression of Akt/mTOR and decreased EGFR. In glioma cells, BIBU 1361 decreased the expression of cyclin E and E2F1, increased the level of p21, and increased cell number at the S and G2/M phase of the cell cycle [2].

The effect of BIBU 1361 in the animal body has not been found.

References:
[1].  Antczak C, Mahida JP, Bhinder B, et al. A High-Content Biosensor-Based Screen Identifies Cell-Permeable Activators and Inhibitors of EGFR Function Implications in Drug Discovery. Journal of biomolecular screening, 2012, 17(7): 885-899.
[2].  Ghildiyal R, Dixit D, Sen E. EGFR inhibitor BIBU induces apoptosis and defective autophagy in glioma cells. Molecular carcinogenesis, 2013, 52(12): 970-982.

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References on BIBU 1361 dihydrochloride

Inhibition of epidermal growth factor receptor activity by two pyrimidopyrimidine derivatives.[Pubmed:15199094]

J Pharmacol Exp Ther. 2004 Nov;311(2):502-9.

Overexpression of the epidermal growth factor receptors (EGFRs) and human epidermal growth factor receptor 2 occurs frequently in human cancers and is associated with aggressive tumor behavior and poor patient prognosis. We have investigated the effects in vitro and in vivo of a new class of inhibitor molecules on the growth of several human cancer cell lines. BIBX1382 [N8-(3-chloro-4-fluoro-phenyl)-N2-(1-methyl-piperidin-4-yl)-pyrimido[5,4-d]pyrimi dine-2,8-diamine] and BIBU1361 [(3-chloro-4-fluoro-phenyl)-[6-(4-diethylaminomethyl-piperidin-1yl)-pyrimido[5,4- d]pyrimidin-4-yl]-amine] are two new selective EGFR kinase inhibitors that do not block the activity of other tyrosine kinases. BIBU1361 blocked epidermal growth factor-induced phosphorylation of EGFR and also prevented downstream responses such as mitogen-activated protein kinase kinase (MAPK/extracellular signal-regulated kinase kinase) and MAPK activation in cells. In accordance with these observations thymidine incorporation into EGFR-expressing KB cells was selectively and potently inhibited by BIBX1382 and BIBU1361 with half-maximally effective doses in the nanomolar range. Oral administration of these compounds inhibited the growth of established human xenografts in athymic mice, including vulval and head and neck squamous cell carcinomas. Tumor growth inhibition by BIBX1382 coincided with reduced pEGFR and Ki-67 levels in vivo, which is in accordance with the expected effect of EGFR inhibitors. Collectively, these results show that the structural class of pyrimidopyrimidines, exemplified here by BIBX1382 and BIBU1361, represents an interesting scaffold for the design of EGFR inhibitors.

Description

Selective inhibitor of EGFR-kinase

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