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Zotiraciclib

Cat. No. M10327
Zotiraciclib Structure
Synonym:

TG02; SB1317

Size Price Availability Quantity
5mg USD 98.1  USD109 In stock
10mg USD 143.1  USD159 In stock
25mg USD 287.1  USD319 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Zotiraciclib (TG02, SB1317) is an orally bioavailable, brain penetrant multi-kinase inhibitor of CDK2, JAK2, and FLT3 with IC50 values of 13, 73, and 56 nM, respectively. Zotiraciclib inhibits cell proliferation concentrations in HCT-116 (IC50=0.079 μM) and HL-60 (IC50=0.059 μM). 

In vivo, treatment with Zotiraciclib (SB1317) at 75 mg/kg po q.d. 3×/week significantly inhibits the growth of tumors with a mean TGI of 82%, while the lower dose of 50 mg/kg po 3×/week is marginally effective. Treatment with Zotiraciclib using either regime significantly inhibits the growth of tumors with mean TGIs of 42% and 63% for the oral and ip delivery methods, respectively.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 372.46
Formula C23H24N4O
CAS Number 1204918-72-8
Purity >99%
Solubility DMSO 20 mg/mL
Storage at -20°C
References

Preclinical metabolism and pharmacokinetics of SB1317 (TG02), a potent CDK/JAK2/FLT3 inhibitor
Mohammed Khalid Pasha, et al. Drug Metab Lett. 2012 Mar;6(1):33-42. PMID: 22372550.

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
Anthony D William, et al. J Med Chem. 2012 Jan 12;55(1):169-96. PMID: 22148278.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Zotiraciclib, TG02; SB1317 supplier, CDK, inhibitors

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