1204918-72-8

Basic information

• Product Name: SB1317
• Synonyms: SB1317;TG02;SB1317 (Double bond E);TG02 (Double bond E);SB1317 (TG-02);VXBAJLGYBMTJCY-UHFFFAOYSA-N
• CAS NO: 1204918-72-8
• Molecular Formula: C23H24N4O
• Molecular Weight: 372.46286
• Product Categories: Inhibitors
• Mol File: 1204918-72-8.mol
• Article Data: 3

Chemical Properties

• Appearance: /
• CAS DataBase Reference: SB1317(CAS DataBase Reference)
• NIST Chemistry Reference: SB1317(1204918-72-8)
• EPA Substance Registry System: SB1317(1204918-72-8)

Safety Data

• Hazardous Substances Data: 1204918-72-8(Hazardous Substances Data)

Usage

Uses

TG 02 is a cyclin dependent kinase inhibitors (CDK inhibitors) for the treatment of chronic lymphocytic leukemia.

Upstream product

• 937271-56-2 3-[(allylmethylamino)methyl]phenylamine 
• 937271-45-9 4-(3-(but-3-en-1-yloxy)phenyl)-2-chloropyrimidine 
• 937271-55-1 allylmethyl-(3-nitrobenzyl)amine 
• 99-61-6 3-nitro-benzaldehyde 
• 156682-54-1 3-(benzyloxy)phenylboronic acid 
• 87199-18-6 3-hydroxyphenylboronic acid 
• 937271-61-9 C₂₅H₂₈N₄O 
• 937271-43-7 3-(2-chloropyrimidine-4-yl)phenol 

Relevant articles and documents

Polymorphic form of TG02

The present disclosure provides crystalline polymorphic forms of TG02 free base and TG02 acid addition salts, pharmaceutical compositions comprising crystalline polymorphic forms of TG02 free base and TG02 acid addition salts, and methods of treating cancer and other diseases in a patient with crystalline polymorphic forms of TG02 free base and TG02 acid addition salts.

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

Herein, we describe the design, synthesis, and SAR of a series of unique small molecule macrocycles that show spectrum selective kinase inhibition of CDKs, JAK2, and FLT3. The most promising leads were assessed in vitro for their inhibition of cancer cell proliferation, solubility, CYP450 inhibition, and microsomal stability. This screening cascade revealed 26h as a preferred compound with target IC50 of 13, 73, and 56 nM for CDK2, JAK2 and FLT3, respectively. Pharmacokinetic (PK) studies of 26h in preclinical species showed good oral exposures. Oral efficacy was observed in colon (HCT-116) and lymphoma (Ramos) xenograft studies, in line with the observed PK/PD correlation. 26h (SB1317/TG02) was progressed into development in 2010 and is currently undergoing phase 1 clinical trials in advanced leukemias and multiple myeloma.