الصفحة الرئيسية>>Signaling Pathways>> Ubiquitination/ Proteasome>> Autophagy>>Bafetinib

Bafetinib (Synonyms: INNO-406)

رقم الكتالوجGC35462

Bafetinib هو مثبط قوي وفعال عن طريق الفم Lyn / Bcr-Abl tyrosine kinaseيعزز Bafetinib أنشطة العديد من البروتينات المتجانسة Bcl-2 (BH) 3 فقط (Bim و Bad و Bmf و Bik) ويحث على موت الخلايا المبرمج في خلايا سرطان الدم Ph + عبر مسار موت الخلايا المبرمج الجوهري Bcl-2 المنظم من قبل الأسرة

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Bafetinib التركيب الكيميائي

Cas No.: 859212-16-1

الحجم السعر المخزون الكميّة
10mM (in 1mL DMSO)
66٫00
متوفر
5mg
52٫00
متوفر
10mg
91٫00
متوفر
50mg
175٫00
متوفر
100mg
315٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of Bafetinib

Bafetinib is a potent and selective dual inhibitor of Bcr-Abl/Lyn tyrosine kinase with IC50 values of 5.8nM and 19nM, respectively [1].

Bafetinib is a specific dual Abl-Lyn inhibitor. For 79 other tyrosine kinases, 0.1μM bafetinib can inhibit 4 of these enzymes including Abl, Abl-related gene, Fyn and Lyn. Bafetinib can block the autophosphorylation of Bcr-Abl. In K562 and 293T cells transfected with wt Bcr-Abl, bafetinib shows inhibition with IC50 values of 11nM and 22nM, respectively. In the in vitro kinase assays, bafetinib shows inhibition of a variety of Abl kinase mutants such as M244V, G250E, Y253F and F317L. It has no effect on T315I in vitro. Bafetinib also suppresses the growth of Bcr-Abl–positive leukemic cell lines including K562, KU812 and BaF3/wt. The BaF3/E255K cells are also sensitive towards bafetinib. Moreover, bafetinib is highly potent to inhibit tumor growth in murine tumor models [1].

References:
[1] Kimura S, Naito H, Segawa H, et al. NS-187, a potent and selective dual Bcr-Abl/Lyn tyrosine kinase inhibitor, is a novel agent for imatinib-resistant leukemia. Blood, 2005, 106(12): 3948-3954.

Protocol of Bafetinib

Kinase experiment [1]:

Kinase assays

Bcr-Abl kinase assays were performed in 25 μL of reaction mixture containing 250 μM peptide substrate, 740 Bq/μL [γ-33P]ATP, and 20 μM cold adenosine triphosphate (ATP) by using the SignaTECT protein tyrosine kinase assay system. Each Bcr-Abl kinase was used at a concentration of 10 nM. Kinase assays for Abl, Src, and Lyn were carried out with an enzyme-linked immunosorbent assay (ELISA) kit from Carna Biosciences.

Cell experiment [1]:

Cell lines

K562, BaF3/wt and KU812 cell lines

Preparation method

The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0-10 μM for 3 days

Applications

Bafetinib could suppress the growth of the Bcr-Abl–positive cell lines K562, KU812, and BaF3/wt.

Animal experiment [1]:

Animal models

Bcr-Abl–positive KU812 mouse model

Dosage form

0.2 mg/kg/d and 20 mg/kg/d orally twice a day for 26 consecutive days

Application

Bafetinib suppressed the growth of Bcr-Abl–bearing tumors (KU812) and markedly extends the survival of mice bearing such tumors.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Kimura S, Naito H, Segawa H, et al. NS-187, a potent and selective dual Bcr-Abl/Lyn tyrosine kinase inhibitor, is a novel agent for imatinib-resistant leukemia. Blood, 2005, 106(12): 3948-3954.

Chemical Properties of Bafetinib

Cas No. 859212-16-1 SDF
المرادفات INNO-406
Chemical Name (S)-N-(3-([4,5'-bipyrimidin]-2-ylamino)-4-methylphenyl)-4-((3-(dimethylamino)pyrrolidin-1-yl)methyl)-3-(trifluoromethyl)benzamide
Canonical SMILES O=C(NC1=CC=C(C)C(NC2=NC=CC(C3=CN=CN=C3)=N2)=C1)C4=CC=C(CN5C[C@@H](N(C)C)CC5)C(C(F)(F)F)=C4
Formula C30H31F3N8O M.Wt 576.62
الذوبان DMSO: ≥ 42 mg/mL (72.84 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Bafetinib

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.7342 mL 8.6712 mL 17.3424 mL
5 mM 0.3468 mL 1.7342 mL 3.4685 mL
10 mM 0.1734 mL 0.8671 mL 1.7342 mL
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3. All of the above co-solvents are available for purchase on the GlpBio website.

Product Documents

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