Art. -Nr.: HY-15163

Zotiraciclib

(Synonyms: TG02; SB1317)

2 Cited Publications

Kundenbewertung

Based on 2 publication(s) in Google Scholar

Zotiraciclib (TG02; SB1317) is an orally active JAK2/FLT3/CDK2 inhibitor with IC₅₀ values of 13 nM, 73 nM and 56 nM, respectively. Zotiraciclib inhibits cancer cell proliferation, tumor growth and the activity of CYP2D6. Zotiraciclib exhibits high plasma protein binding rate, Caco-2 permeability and tissue distribution capacity, as well as metabolic stability in human and canine liver microsomes. Zotiraciclib achieves tumor growth inhibition in nude mouse models of colon cancer and lymphoma xenografts. Zotiraciclib can be used for research related to colon cancer, B-cell lymphoma, advanced leukemia, acute leukemia and multiple myeloma.

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Reinheit: 99.88%
CAS. Nr.: 1204918-72-8
Formel: C₂₃H₂₄N₄O
Molecular Weight:372.46

Speicherung:

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

Zotiraciclib Chemical Structure

CAS. Nr.: 1204918-72-8

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
- Clinical Trial
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

CDK2

56 nM (IC₅₀)

JAK2

13 nM (IC₅₀)

Alle JAK Isoform-spezifische Produkte anzeigen :

Alle CDK Isoform-spezifische Produkte anzeigen :

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

Zotiraciclib (up to 10 μM; 48 h) potently inhibits proliferation of HL-60, HCT-116, Ramos, COLO205, and DU145 cancer cell lines with IC₅₀ values ranging from 0.033 μM to 0.14 μM^[1].
Zotiraciclib (8-1000 nM; 24 h) inhibits phospho-Rb in HCT-116 cells, with detectable effects at 40 nM and complete inhibition at 200 nM after 24 h of treatment^[1].
Zotiraciclib (0.05-25 μM; 5-60 min depending on isoform) inhibits human CYP2D6 with an IC₅₀ of 0.95 μM, but does not inhibit CYP1A2, 2C9, 2C19, or 3A4 at concentrations up to 25 μM^[1].
Zotiraciclib (5 μM; 120 min) exhibits high permeability with low efflux across Caco-2 cell monolayers, with Papp values of 28.0 × 10^-6 cm/s (apical-to-basolateral) and 27.4 × 10^-6 cm/s (basolateral-to-apical) at 5 μM for 120 min^[2].

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, DU145
Concentration:

0-10 μM (IC₅₀ values); up to 10 μM
Incubation Time:

48 h
Result:

Inhibited HL-60 cell proliferation with an IC₅₀ of 0.059 μM.
Inhibited HCT-116 cell proliferation with an IC₅₀ of 0.079 μM.
Inhibited Ramos cell proliferation with an IC₅₀ of 0.033 μM.
Inhibited COLO205 cell proliferation with an IC₅₀ of 0.072 μM.
Inhibited DU145 cell proliferation with an IC₅₀ of 0.14 μM.

Western Blot Analysis^[1]

Cell Line:

HCT-116
Concentration:

8, 40, 200, 1000 nM
Incubation Time:

24 h
Result:

Inhibited phospho-Rb detectably at 40 nM.
Achieved complete inhibition of phospho-Rb at 200 nM.

Parmacokinetics

Species	Dose	Route	CL	V_ss	T_1/2	AUC_0-t	AUC_0-∞	Bioavailability	T_max	C_max	CL/F	V_d/F
Mice^[1]	75 mg/kg	p.o.	/	/	6.1 h	/	2523 ng·h/mL	24 %	0.5 h	1029 ng/mL	/	/
Dog^[1]	10 mg/kg	p.o.	/	/	/	/	/	4 %	/	/	/	/
Rat^[1]	10 mg/kg	p.o.	/	/	/	/	/	37 %	/	/	/	/
Mice^[2]	5 mg/kg	i.v.	6.6 L/h/kg	23 L/kg	4.6 h	732 ng·h/mL	752 ng·h/mL	/	/	/	/	/
Mice^[2]	75 mg/kg	p.o.	/	/	6.1 h	2523 ng·h/mL	2700 ng·h/mL	24 %	0.5 h	1029 ng/mL	28 L/h/kg	245 L/kg
Rat^[2]	2 mg/kg	i.v.	2.4 L/h/kg	1.80 L/kg	1.4 h	897 ng·h/mL	916 ng·h/mL	/	/	/	/	/
Rat^[2]	10 mg/kg	p.o.	/	/	/	172 ± 38 ng·h/mL	/	3.8 %	0.08 ± 0.0 h	62 ± 25 ng/mL	/	/
Dog^[2]	1 mg/kg	i.v.	1.1 L/h/kg	3.1 L/kg	2.9 h	819 ng·h/mL	900 ng·h/mL	/	/	/	/	/
Dog^[2]	5 mg/kg	p.o.	/	/	2.9 h	1659 ng·h/mL	1663 ng·h/mL	37 %	1.0 h	493 ng/mL	3.0 L/h/kg	12.6 L/kg

In Vivo

Zotiraciclib (50-75 mg/kg; p.o.; 3 times per week; 15 days) administered orally at 75 mg/kg 3 times per week achieves a mean tumor growth inhibition of 82% in HCT-116 colon cancer xenografts in nude mice^[1].
Zotiraciclib (15-75 mg/kg; p.o., i.p.; once daily, 2 days on/5 days off, 5 days on/5 days off; 14 days) administered orally at 75 mg/kg on a 2 days on/5 days off schedule achieves 42% TGI, and intraperitoneally at 15 mg/kg on a 5 days on/5 days off schedule achieves 63% TGI in Ramos B-cell lymphoma xenografts in nude mice^[1].

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

Animal Model:

BALB/c nude mice (female, 10−12 weeks of age)^[1]
Dosage:

50 mg/kg; 75 mg/kg
Administration:

p.o.; 3 times per week (Monday, Wednesday, Friday); 15 days
Result:

Achieved a mean tumor growth inhibition (TGI) of 82% (75 mg/kg).
Was marginally effective (50 mg/kg).

Animal Model:

BALB/c nude mice (female, 10−12 weeks of age)^[1]
Dosage:

75 mg/kg (TGI 42%); 15 mg/kg (TGI 63%)
Administration:

p.o.; once daily, 2 days on and 5 days off schedule; 14 days; i.p.; once daily, 5 days on and 5 days off schedule
Result:

Achieved a mean TGI of 42% (75 mg/kg, oral, 2 days on/5 days off schedule).
Achieved a mean TGI of 63% (15 mg/kg, intraperitoneal, 5 days on/5 days off schedule).

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1204918-72-8
Appearance Solid
Molecular Weight 372.46
Formel C₂₃H₂₄N₄O
Color White to off-white
SMILES

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

TG02; SB1317
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (2)

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Journal Impact Factor

Mol Cancer Ther

Inhibition of CDKs Enhances Efficacy of Anti-EGFR Therapy in Chordoma. [Abstract]

2025 Dec 4. PMID: 41340469
University of Washington

2025.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (268.49 mM; Need ultrasonic; 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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: ≥ 2.5 mg/mL (6.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (396 KB)
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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)

Verweise

[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 kinases (CDKs), Janus kinase 2 (JAK2), and fms-like tyrosine kinase-3 (FLT3) for the treatment of cancer. J Med Chem. 2012 Jan 12;55(1):169-96. [Content Brief]

[2]. Pasha MK, et al. Preclinical metabolism and pharmacokinetics of SB1317 (TG02), a potent CDK/JAK2/FLT3 inhibitor. Drug Metab Lett. 2012;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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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
	80 mM	0.0336 mL	0.1678 mL	0.3356 mL	0.8390 mL
	100 mM	0.0268 mL	0.1342 mL	0.2685 mL	0.6712 mL

Zotiraciclib

2 Cited Publications

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Zotiraciclib

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

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Publications Citing Use of MedChemExpress (MCE) Zotiraciclib

Alle JAK Isoform-spezifische Produkte anzeigen

Alle CDK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Zotiraciclib Related Classifications

HY-15163 Related Classifications