A LCK kinase inhibitor
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A-770041

Item No. 32854

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[1-[trans-4-(4-acetyl-1-piperazinyl)cyclohexyl]-4-amino-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-2-methoxyphenyl]-1-methyl-1H-indole-2-carboxamide
CAS Number
869748-10-7
Molecular Formula
C34H39N9O3
Formula Weight
621.7
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
0.1 M HCl: 20 mg/mlDMSO: 20 mg/mlEthanol: 2 mg/ml
SMILES
NC1=C2C(C3=CC(OC)=C(C=C3)NC(C4=CC5=CC=CC=C5N4C)=O)=NN([C@@]6([H])CC[C@@](N7CCN(CC7)C(C)=O)([H])CC6)C2=NC=N1
InChi Code
InChI=1S/C34H39N9O3/c1-21(44)41-14-16-42(17-15-41)24-9-11-25(12-10-24)43-33-30(32(35)36-20-37-33)31(39-43)23-8-13-26(29(19-23)46-3)38-34(45)28-18-22-6-4-5-7-27(22)40(28)2/h4-8,13,18-20,24-25H,9-12,14-17H2,1-3H3,(H,38,45)(H2,35,36,37)/t24-,25-
InChi Key
ZMNWFTYYYCSSTF-SOAUALDESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $63

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    $213

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    Product Description

    A-770041 is an inhibitor of LCK kinase (IC50 = 0.147 µM).1 It is selective for LCK over other Src family tyrosine kinases including Src, Fyn, Fgr, HCK, and Tie2 (IC50s = 9.05, 44.1, 14.1, 1.22, and >50 µM, respectively). A-770041 induces dephosphorylation of LCK by SHP-1, inactivating LCK, in IgE/antigen-stimulated bone marrow-derived mast cells (BMMCs).2 It inhibits IL-2 production induced by an anti-CD3 antibody and phorbol 12-myristate 13-acetate (PMA; Item No. 10008014) in isolated human whole blood (EC50 = 80 nM) and by concanavalin A (Item No. 14951) in rats.3 A-770041 (10 mg/kg) prevents acute rejection and increases graft survival in a rat model of heterotopic heart transplantation. It also inhibits the growth of CTV-1 human acute myeloid leukemia cells (IC50 = 224 nM) and sensitizes U2OSMR and KHOSR2 multidrug resistant human osteosarcoma cells to paclitaxel (Item No. 10461) and doxorubicin (Item No. 15007).4,5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Burchat, A., Borhani, D.W., Calderwood, D.J., et al. Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection. Bioorg. Med. Chem. Lett. 16(1), 118-122 (2006).

    2. Chang, H.W., Kanegasaki, S., Jin, F., et al. A common signaling pathway leading to degranulation in mast cells and its regulation by CCR1-ligand. Allergy 75(6), 1371-1381 (2020).

    3. Stachlewitz, R.F., Hart, M.A., Bettencourt, B., et al. A-770041, a novel and selective small-molecule inhibitor of Lck, prevents heart allograft rejection. J. Pharmacol. Exp. Ther. 315(1), 36-41 (2005).

    4. Li, L., Cui, Y., Shen, J., et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1. Leuk. Res. 78, 12-20 (2019).

    5. Duan, Z., Zhang, J., Ye, S., et al. A-770041 reverses paclitaxel and doxorubicin resistance in osteosarcoma cells. BMC Cancer 14, 681 (2014).