1. Cell Cycle/DNA Damage Protein Tyrosine Kinase/RTK JAK/STAT Signaling Epigenetics Stem Cell/Wnt
  2. CDK JAK FLT3
  3. (E/Z)-Zotiraciclib

(E/Z)-Zotiraciclib  (Synonyms: (E/Z)-TG02; (E/Z)-SB1317)

Cat. No.: HY-15166 Purity: 99.70%
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(E/Z)-Zotiraciclib ((E/Z)-TG02) is a potent inhibitor of CDK2, JAK2 and FLT3 with IC50s of 13, 73 and 56 nM, respectively. (E/Z)-Zotiraciclib effectively inhibits the proliferation of cancer cells, it can be used for the research of cancer.

For research use only. We do not sell to patients.

(E/Z)-Zotiraciclib Chemical Structure

(E/Z)-Zotiraciclib Chemical Structure

CAS No. : 937270-47-8

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10 mM * 1 mL in DMSO
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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of (E/Z)-Zotiraciclib:

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Description

(E/Z)-Zotiraciclib ((E/Z)-TG02) is a potent inhibitor of CDK2, JAK2 and FLT3 with IC50s of 13, 73 and 56 nM, respectively. (E/Z)-Zotiraciclib effectively inhibits the proliferation of cancer cells, it can be used for the research of cancer[1][2].

IC50 & Target[1]

CDK2

13 nM (IC50)

JAK2

73 nM (IC50)

FLT3

56 nM (IC50)

In Vitro

(E/Z)-Zotiraciclib (0-10 μM) shows potent inhibition to CDK2, JAK2 and FLT3 with IC50s of 13, 73 and 56 nM, respectively[1].
? (E/Z)-Zotiraciclib (0-10 μM; 48 h) inhibits proliferation of cancer cells[1].
? (E/Z)-Zotiraciclib (8-1000 nM; 24 h) potently inhibits the CDK2 biomarker pRb in HCT-116 cells and potently againsts pRb in MV4-11 cells with an IC50 value of 0.13 μM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: HL-60, HCT-116, RAMOS, COLO205 and DU145 cell lines
Concentration: 0-10 μM
Incubation Time: 48 h
Result: Inhibited proliferation of HL-60, HCT-116, RAMOS, COLO205 and DU145 cells with IC50s of 0.059, 0.079, 0.033, 0.072 and 0.14 μM, respectively.
In Vivo

(E/Z)-Zotiraciclib (50 and 75 mg/kg; p.o. once daily for 3 weeks) inhibits tumor growth[1].
? (E/Z)-Zotiraciclib (15 and 75 mg/kg; p.o. once daily 2 days on and 5 days off; i.p. once daily 5 days on 5 days off) inhibits tumor growth in two manners[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male BALB/c mice with HCT-116 colon cancer cells xenografts[1]
Dosage: 50 and 75 mg/kg
Administration: Oral gavage; 50 and 75 mg/kg once daily for 3 weeks
Result: Significantly inhibited the growth of tumors with a mean TGI of 82%.
Animal Model: Male BALB/c mice with lymphoma Ramos cells xenografts[1]
Dosage: 15 and 75 mg/kg
Administration: Oral gavage and intraperitoneal injection ; 75 mg/kg once daily 2 days on and 5 days off (p.o.) and 15 mg/kg once daily 5 days on 5 days off (i.p.)
Result: Significantly inhibited the growth of tumors with mean TGIs of 42% and 63% for the oral and ip delivery methods, respectively.
Molecular Weight

372.46

Formula

C23H24N4O

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CN1CC2=CC(NC3=NC(C4=CC(OCC/C=C/C1)=CC=C4)=CC=N3)=CC=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

DMSO : 26.5 mg/mL (71.15 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6849 mL 13.4243 mL 26.8485 mL
5 mM 0.5370 mL 2.6849 mL 5.3697 mL
10 mM 0.2685 mL 1.3424 mL 2.6849 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (5.58 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (5.58 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (5.58 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.96%

References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
(E/Z)-Zotiraciclib
Cat. No.:
HY-15166
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