Fig. 1 · Structure

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(E/Z)-Zotiraciclib ((E/Z)-TG-02, (E/Z)-SB1317)

Cat. No. A11962 CAS 937270-47-8

FLT3 inhibitor

TG-02 is a novel small molecule potent CDK/JAK2/FLT3 inhibitor.

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Biological Activity

Cellular Effect

Cell Line Activity Value Description Reference
COLO 205 IC50 0.072 μM Antiproliferative activity against human COLO205 cells after 48 hrs [PMID: 22148278]
DU-145 IC50 0.14 μM Antiproliferative activity against human DU145 cells after 48 hrs [PMID: 22148278]
HCT-116 IC50 0.079 μM Antiproliferative activity against human HCT116 cells after 48 hrs [PMID: 22148278]
HEL GI50 0.79 μM Antiproliferative activity against human HEL cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay [PMID: 25800646]
HL-60 IC50 0.059 μM Antiproliferative activity against human HL60 cells after 48 hrs [PMID: 22148278]
HL-60 GI50 1.13 μM Antiproliferative activity against human HL60 cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay [PMID: 25800646]
K562 GI50 1.23 μM Antiproliferative activity against human K562 cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay [PMID: 25800646]
MV4-11 IC50 0.13 μM Inhibition of CDK2 in human MV411 cells assessed as Rb phosphorylation after 24 hrs by Western blot analysis [PMID: 22148278]
MV4-11 GI50 0.66 μM Antiproliferative activity against human MV4-11 cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay [PMID: 25800646]
Ramos IC50 0.033 μM Antiproliferative activity against human Ramos cells after 48 hrs [PMID: 22148278]
Sf21 IC50 37 nM Inhibition of recombinant human C-terminal His6-tagged full length CDK7/untagged recombinant full length human Cyclin H/N-terminal GST-tagged recombinant full length human MAT1 expressed in baculovirus infected Sf21 insect cells using cdk7 peptide as subs [PMID: 30543440]
Sf21 IC50 8 nM Inhibition of recombinant human full-length C-terminal His6-tagged CDK3/full-length human N-terminal GST-tagged Cyclin E expressed in baculovirus infected Sf21 insect cells using histone H1 as substrate [PMID: 30543440]

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Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 937270-47-8
Applications FLT3 inhibitor
Formula C23H24N4O
Molecular Weight 372.46
Synonyms TG 02; SB1317; (E/Z)-TG-02; (E/Z)-SB1317
SMILES
CN1C/C=C/CCOC2=CC=CC(=C2)C3=NC(=NC=C3)NC4=CC=CC(=C4)C1

Storage & Solubility

In Vitro Solubility

Reported Solubility

No reported solubility data are available for this product.

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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