Doramapimod (BIRB 796)

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Chemical Information

Product name：Doramapimod (BIRB 796)	Purity：98% min
CAS NO：285983-48-4	Solubility：DMSO : ≥ 100 mg/mL (189.52 mM)
Molecular Formula：C₃₁H₃₇N₅O₃	Package：Packaging according to customer requirements
Molecular Weight：527.657	Storage：Store at -20℃

Quality control

Remarks

Doramapimod (BIRB 796) is a pan-p38 MAPK inhibitor with IC50 of 38 nM, 65 nM, 200 nM and 520 nM for p38α/β/γ/δ in cell-free assays, and binds p38α with Kd of 0.1 nM in THP-1 cells, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2.

Properties:

Density: 1.2g/cm3

Boiling Point: 631.6ºC at 760mmHg

Flash Point: 335.8ºC

Refractive Index: 1.619

Vapor Pressure: 7.36E-16mmHg at 25°C

Raf Inhibitors Related Products:

Vemurafenib; PLX-4720; Debrafenib; Regorafenib; GDC-0879; RAF265 (CHIR-265); AZ-628; SB590885; ZM 336372; TAK-632; B-Raf IN 1; AZ304; Dabrafenib Mesylate; RAF709; LY3009120; RO5126766; MLN2480 ; GW5074

References

[1]. Dietrich J, et al. The design, synthesis, and evaluation of 8 hybrid DFG-out allosteric kinase inhibitors: a structural analysis of the binding interactions of Gleevec, Nexavar, and BIRB-796. Bioorg Med Chem. 2010 Aug 1;18(15):5738-48

[2]. Pargellis C, et al. Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site. Nat Struct Biol, 2002, 9(4), 268-272.