An FLT3 inhibitor
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FLT3-IN-3

Item No. 36106

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N2-(trans-4-aminocyclohexyl)-9-cyclopentyl-N6-[4-(4-morpholinylmethyl)phenyl]-9H-purine-2,6-diamine
CAS Number
2229050-90-0
Synonyms
  • SAN50900
Molecular Formula
C27H38N8O
Formula Weight
490.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/mlEthanol: 15 mg/mlPBS (pH 7.2): insol
λmax
262, 312 nm
SMILES
N[C@H](CC1)CC[C@@H]1NC2=NC(NC3=CC=C(C=C3)CN4CCOCC4)=C5C(N(C6CCCC6)C=N5)=N2
InChi Code
InChI=1S/C27H38N8O/c28-20-7-11-22(12-8-20)31-27-32-25(24-26(33-27)35(18-29-24)23-3-1-2-4-23)30-21-9-5-19(6-10-21)17-34-13-15-36-16-14-34/h5-6,9-10,18,20,22-23H,1-4,7-8,11-17,28H2,(H2,30,31,32,33)/t20-,22-
InChi Key
SAEGVASGMTZGFI-AQYVVDRMSA-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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    5 mg

    $325

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    10 mg

    $546

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    25 mg

    $1,023

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    Product Description

    FLT3-IN-3 is an inhibitor of FMS-related tyrosine kinase 3 (FLT3).1 It inhibits wild-type, FLT3D835Y, and FLT3 bearing internal-tandem duplication (FLT3-ITD; IC50s = 13, 8, and 3 nM, respectively). FLT3-IN-3 suppresses the growth of MV4-11 acute myeloid leukemia (AML) cells that express FLT3-ITD (GI50 = 7 nM). It induces cell cycle arrest at the G1 phase and apoptosis in the same cells. FLT3-IN-3 (10 mg/kg) reduces intratumor FLT3-ITD autophosphorylation in a MV4-11 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gucký, T., E., Ř., Radošová Muchová, T., et al. Discovery of N2-(4-amino-cyclohexyl)-9-cyclopentyl- N6-(4-morpholin-4-ylmethyl-phenyl)- 9H-purine-2,6-diamine as a potent FLT3 kinase inhibitor for acute myeloid leukemia with FLT3 mutations. J. Med. Chem. 61(90), 3855-3869 (2018).