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SB1317

Cat. No. M2239
SB1317 Structure
Synonym:

TG02

Size Price Availability Quantity
5mg USD 95  USD95 In stock
10mg USD 140  USD140 In stock
25mg USD 300  USD300 In stock
50mg USD 425  USD425 In stock
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Quality Control & Documentation
Biological Activity

SB1317 (TG02) is a novel pyrimidine-based multi-kinase inhibitor that inhibits CDKs 1, 2, 7 and 9 together with JAK2 and FLT3. SB1317 dose-dependently inhibits signaling pathways downstream of CDKs, JAK2 and FLT3 in cancer cells with the main targets being CDKs. SB1317 induces tumor regression after oral dosing on both daily and intermittent schedules in a murine model of mutant-FLT3 leukemia (MV4-11) and prolongs survival in a disseminated AML model with wild-type FLT3 and JAK2 (HL-60). In vivo, SB1317 (TG02) exhibits favorable pharmacokinetics after oral dosing in xenograft models and accumulates in tumor tissues, inducing an effective blockade of both CDK and STAT signaling. SB1317 is currently undergoing phase 1 clinical trials in advanced leukemias and multiple myeloma.

Chemical Information
Molecular Weight 372.46
Formula C23H24N4O
CAS Number 937270-47-8
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Yu-Ting Su, et al. Novel Targeting of Transcription and Metabolism in Glioblastoma

[2] Anthony D William, et al. Acid Mediated Ring Closing Metathesis: A Powerful Synthetic Tool Enabling the Synthesis of Clinical Stage Kinase Inhibitors

[3] Anders Poulsen, et al. Structure-based design of nitrogen-linked macrocyclic kinase inhibitors leading to the clinical candidate SB1317/TG02, a potent inhibitor of cyclin dependant kinases (CDKs), Janus kinase 2 (JAK2), and Fms-like tyrosine kinase-3 (FLT3)

[4] Mohammed Khalid Pasha, et al. Preclinical metabolism and pharmacokinetics of SB1317 (TG02), a potent CDK/JAK2/FLT3 inhibitor

[5] Anthony D William, 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 k䲧畸Ỵ畹㧀畷羹皖睑ꏰऒŤऒĀ�皘嶁皔Ѐ瑖徿䀹ࣵ

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  Catalog
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Keywords: SB1317, TG02 supplier, CDK, inhibitors, activators


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