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.
Cell Signal. 2024 Jan ;8;115:111040.
MBIP promotes ESCC metastasis by activating MAPK pathway
BIRB796 purchased from AbMole
Cell Experiment | |
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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 | |
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Animal models | Male Crlj:CD1(ICR)mice |
Formulation | saline |
Dosages | 250, 500 or 1000 mg/kg |
Administration | oral |
Molecular Weight | 527.66 |
Formula | C31H37N5O3 |
CAS Number | 285983-48-4 |
Solubility (25°C) | DMSO 66 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
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