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Reagents and instruments for immunology, cell biology and molecular biology.

(E/Z)-Zotiraciclib [937270-47-8]

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Cat# HY-15166-5mg

Size : 5mg

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Brand : MedChemExpress

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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)

Cellular Effect

Cell Line	Type	Value	Description	References
COLO 205	IC₅₀	0.072 μM Compound: 26h, SB1317/TG02	Antiproliferative activity against human COLO205 cells after 48 hrs Antiproliferative activity against human COLO205 cells after 48 hrs	[PMID: 22148278]
DU-145	IC₅₀	0.14 μM Compound: 26h, SB1317/TG02	Antiproliferative activity against human DU145 cells after 48 hrs Antiproliferative activity against human DU145 cells after 48 hrs	[PMID: 22148278]
HCT-116	IC₅₀	0.079 μM Compound: 26h, SB1317/TG02	Antiproliferative activity against human HCT116 cells after 48 hrs Antiproliferative activity against human HCT116 cells after 48 hrs	[PMID: 22148278]
HEL	GI₅₀	0.79 μM Compound: SB1317	Antiproliferative activity against human HEL cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay Antiproliferative activity against human HEL cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay	[PMID: 25800646]
HL-60	GI₅₀	1.13 μM Compound: SB1317	Antiproliferative activity against human HL60 cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay Antiproliferative activity against human HL60 cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay	[PMID: 25800646]
HL-60	IC₅₀	0.059 μM Compound: 26h, SB1317/TG02	Antiproliferative activity against human HL60 cells after 48 hrs Antiproliferative activity against human HL60 cells after 48 hrs	[PMID: 22148278]
K562	GI₅₀	1.23 μM Compound: SB1317	Antiproliferative activity against human K562 cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay Antiproliferative activity against human K562 cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay	[PMID: 25800646]
MV4-11	GI₅₀	0.66 μM Compound: SB1317	Antiproliferative activity against human MV4-11 cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay Antiproliferative activity against human MV4-11 cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay	[PMID: 25800646]
MV4-11	IC₅₀	0.13 μM Compound: 26h, SB1317/TG02	Inhibition of CDK2 in human MV411 cells assessed as Rb phosphorylation after 24 hrs by Western blot analysis Inhibition of CDK2 in human MV411 cells assessed as Rb phosphorylation after 24 hrs by Western blot analysis	[PMID: 22148278]
Ramos	IC₅₀	0.033 μM Compound: 26h, SB1317/TG02	Antiproliferative activity against human Ramos cells after 48 hrs Antiproliferative activity against human Ramos cells after 48 hrs	[PMID: 22148278]
Sf21	IC₅₀	37 nM Compound: TG02	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 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 Compound: TG02	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 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]

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.

937270-47-8

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.58 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Purity & Documentation

Purity: 99.96%

Data Sheet (283 KB) SDS (392 KB)

COA (255 KB) HNMR (211 KB) LCMS (121 KB)

Handling Instructions (2659 KB)

References

[1]. William AD, et al. Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kina [Content Brief]

[2]. Pasha MK, et al. Preclinical metabolism and pharmacokinetics of SB1317 (TG02), a potent CDK/JAK2/FLT3 inhibitor. Drug Metab Lett. 2012 Mar;6(1):33-42. [Content Brief]

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(E/Z)-Zotiraciclib [937270-47-8]

Cat# HY-15166-5mg

Contact local distributor :

Brand : MedChemExpress

Contact local distributor :

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