An allosteric inhibitor of Abl1
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Asciminib

Item No. 26126

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-(chlorodifluoromethoxy)phenyl]-6-[(3R)-3-hydroxy-1-pyrrolidinyl]-5-(1H-pyrazol-3-yl)-3-pyridinecarboxamide
CAS Number
1492952-76-7
Synonyms
  • ABL001
Molecular Formula
C20H18ClF2N5O3
Formula Weight
449.8
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: >90 mg/mlEthanol: >90 mg/ml
λmax
317 nm
SMILES
O=C(NC1=CC=C(OC(F)(F)Cl)C=C1)C2=CN=C(N3C[C@H](O)CC3)C(C4=NNC=C4)=C2
InChi Code
InChI=1S/C20H18ClF2N5O3/c21-20(22,23)31-15-3-1-13(2-4-15)26-19(30)12-9-16(17-5-7-25-27-17)18(24-10-12)28-8-6-14(29)11-28/h1-5,7,9-10,14,29H,6,8,11H2,(H,25,27)(H,26,30)/t14-/m1/s1
InChi Key
VOVZXURTCKPRDQ-CQSZACIVSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $69

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    $525

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    Product Description

    Asciminib is an allosteric inhibitor of Abl1 (IC50 = 0.45 nM).1 It is selective for Abl1 over a panel of more than 60 additional kinases (IC50s = >10 μM), as well as ion channels, nuclear receptors, G protein-coupled receptors (GPCRs), and transporters. Asciminib inhibits the proliferation of Luc-Ba/F3 cells transformed with wild-type Bcr-Abl1 or the drug-resistant mutant Bcr-Abl1T315I (GI50s = 1 and 25 nM, respectively), as well as other drug-resistant mutants.2 It reduces tumor growth in a KCL-22 chronic myelogenous leukemia (CML) mouse xenograft model when administered at a dose of 3 mg/kg twice per day and induces tumor regression at doses of greater than or equal to 7.5 mg/kg twice per day.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wylie, A.A., Schoepfer, J., Jahnke, W., et al. The allosteric inhibitor ABL001 enables dual targeting of BCR-ABL1. Nature 543(7647), 733-737 (2017).

    2. Schoepfer, J., Jahnke, W., Berellini, G., et al. Discovery of asciminib (ABL001), an allosteric inhibitor of the tyrosine kinase activity of BCR-ABL1. J. Med. Chem. 61(18), 8120-8135 (2018).