An inhibitor of FLT3
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CHMFL-FLT3-122

Item No. 43137

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-2-(dimethylamino)-ethanone
CAS Number
1839150-56-9
Synonyms
  • HYML-122
Molecular Formula
C26H29N7O2
Formula Weight
471.6
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Slightly soluble: 0.1-1 mg/ml
SMILES
NC1=C2C(C3=CC=C(C=C3)OC4=CC=CC=C4)=NN([C@H]5CN(C(CN(C)C)=O)CCC5)C2=NC=N1
InChi Code
InChI=1S/C26H29N7O2/c1-31(2)16-22(34)32-14-6-7-19(15-32)33-26-23(25(27)28-17-29-26)24(30-33)18-10-12-21(13-11-18)35-20-8-4-3-5-9-20/h3-5,8-13,17,19H,6-7,14-16H2,1-2H3,(H2,27,28,29)/t19-/m1/s1
InChi Key
IZNAFSDUTMZGSF-LJQANCHMSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    CHMFL-FLT3-122 is an inhibitor of FMS-related tyrosine kinase 3 (FLT3; IC50 = 40 nM).1 It is selective for FLT3 over Bruton’s tyrosine kinase (BTK) and C-Kit (IC50s = 421 and 559 nM, respectively) and a panel of 468 additional kinases at 1 µM. CHMFL-FLT3-122 inhibits the growth of MV4-11, MOLM-13, and MOLM-14 acute myeloid leukemia (AML) cells containing FLT3 bearing an internal-tandem duplication (FLT3-ITD; GI50s = 22, 21, and 42 nM, respectively). In vivo, CHMFL-FLT3-122 (50 mg/kg) inhibits tumor growth in an MV4-11 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Li, X., Wang, A., Yu, K., et al. Discovery of (R)-1-(3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)-2-(dimethylamino)ethanone (CHMFL-FLT3-122) as a potent and orally available FLT3 kinase inhibitor for FLT3-ITD positive acute myeloid leukemia. J. Med. Chem. 58(24), 9625-9638 (2015).