Cat. No.: HY-15166

(E/Z)-Zotiraciclib

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

6 Cited Publications

고객리뷰

Based on 6 publication(s) in Google Scholar

(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.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity: 99.70%
CAS No.: 937270-47-8
화학식: C₂₃H₂₄N₄O
분자량:372.46

보관:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

(E/Z)-Zotiraciclib Chemical Structure

CAS No.: 937270-47-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (6)
용액&용해도
- In Vitro
- In Vivo
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[1]

CDK2

13 nM (IC₅₀)

JAK2

73 nM (IC₅₀)

FLT3

56 nM (IC₅₀)

All CDK Isoforms :

All JAK Isoforms :

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.

Chemical Information

CAS No. 937270-47-8
Appearance Solid
분자량 372.46
화학식 C₂₃H₂₄N₄O
Color Off-white to light yellow
SMILES

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

(E/Z)-TG02; (E/Z)-SB1317
선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (6)

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Journal Impact Factor

Science

The target landscape of clinical kinase drugs. [Abstract]

2017 Dec 1;358(6367):eaan4368. PMID: 29191878
Adv Sci (Weinh)

Targeting CDK2 Confers Vulnerability to Lenvatinib Via Driving Senescence in Anaplastic Thyroid Cancer. [Abstract]

2025 Feb;12(7):e2413514. PMID: 39716890
Mol Cancer Res

Inhibition of O-GlcNAc Transferase Renders Prostate Cancer Cells Dependent on CDK9. [Abstract]

2020 Oct;18(10):1512-1521. PMID: 32611550
Cancers (Basel)

Identification of New Vulnerabilities in Conjunctival Melanoma Using Image-Based High Content Drug Screening. [Abstract]

2022 Mar 19;14(6):1575. PMID: 35326726
ACS Chem Biol

Conformational Adaption May Explain the Slow Dissociation Kinetics of Roniciclib (BAY 1000394), a Type I CDK Inhibitor with Kinetic Selectivity for CDK2 and CDK9. [Abstract]

2016 Jun 17;11(6):1710-9. PMID: 27090615
J Neurosurg Pediatr

Targeting of cyclin-dependent kinases in atypical teratoid rhabdoid tumors with multikinase inhibitor TG02. [Abstract]

2021 Sep 3;28(6):734-743. PMID: 34479190

용액&용해도

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6849 mL	13.4243 mL	26.8485 mL	67.1213 mL
	5 mM	0.5370 mL	2.6849 mL	5.3697 mL	13.4243 mL
	10 mM	0.2685 mL	1.3424 mL	2.6849 mL	6.7121 mL
	15 mM	0.1790 mL	0.8950 mL	1.7899 mL	4.4748 mL
	20 mM	0.1342 mL	0.6712 mL	1.3424 mL	3.3561 mL
	25 mM	0.1074 mL	0.5370 mL	1.0739 mL	2.6849 mL
	30 mM	0.0895 mL	0.4475 mL	0.8950 mL	2.2374 mL
	40 mM	0.0671 mL	0.3356 mL	0.6712 mL	1.6780 mL
	50 mM	0.0537 mL	0.2685 mL	0.5370 mL	1.3424 mL
	60 mM	0.0447 mL	0.2237 mL	0.4475 mL	1.1187 mL

Keywords

(E/Z)-Zotiraciclib

6 Cited Publications

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(E/Z)-Zotiraciclib

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Publications Citing Use of MedChemExpress (MCE) (E/Z)-Zotiraciclib

All CDK Isoforms

All JAK Isoforms

Biological Activity

Chemical Information

Publications (6)

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

(E/Z)-Zotiraciclib Related Classifications

HY-15166 Related Classifications