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BIRB796

Cat. No. M1675

BIRB796 Structure

Synonym: Doramapimod

Size Price Availability Quantity
50mg USD 130 In stock
100mg USD 190 In stock
200mg USD 320 In stock
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Quality Control
Biological Activity

BIRB 796 (Doramapimod) is a protein kinase inhibitor of p38 MAPK. BIRB 796 (Doramapimod) has high picomolar affinity (Kd = 100 pM) for p38 MAP kinase and low nanomolar inhibitory activity (IC50 = 18 nM) against TNFα in THP-1 cell culture. The p38 inhibitor BIRB 796 (Doramapimod) binds tightly (Kd = 40 nM) to ABL (T315I) and inhibits the BMS-354825- and imatinib-resistant ABL (T315I) kinase.

Protocol
Cell Experiment
Cell lines MM derived cell line
Preparation method Growth inhibition assay. The growth inhibitory effect of BIRB 796 on MM cell line growth was assessed by measuring 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrasodium bromide (MTT, Sigma Chem-ical) dye absorbance, as previously described (Yasui et al,2005a)
Concentrations 0, 100, 400nM
Incubation time 72h
Animal Experiment
Animal models Male Crlj:CD1(ICR)mice
Formulation saline
Dosages 250, 500 or 1000 mg/kg
Administration oral
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 527.66
Formula C31H37N5O3
CAS Number 285983-48-4
Purity >99%
Solubility DMSO 100 mg/mL
Storage at -20°C
References

Role of p38 mitogen-activated protein kinase in posttraumatic immunosuppression in mice.
Ding et al. J Trauma Acute Care Surg. 2012 Aug 20. PMID: 22914078.

A possible mechanism for hepatotoxicity induced by BIRB-796, an orally active p38 mitogen-activated protein kinase inhibitor.
Iwano et al. J Appl Toxicol. 2011 Oct;31(7):671-7. PMID: 21328587.

X-ray crystal structure of JNK2 complexed with the p38alpha inhibitor BIRB796: insights into the rational design of DFG-out binding MAP kinase inhibitors.
Kuglstatter et al. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5217-20. PMID: 20655210.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: BIRB796, Doramapimod supplier, p38 MAPK, inhibitors

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