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Products are for research use only. Not for human use. We do not sell to patients.

Signaling Pathway

SB1317

HY-15166

(TG02; SB 1317; TG 02; SB-1317; TG-02)

SB1317

SB1317 Chemical Structure

SB1317(TG-02) is a novel small molecule potent CDK2/JAK2/FLT3 inhibitor with IC50s of 13/73/56 nM respectively.

Size Price Stock Quantity
10 mM * 1 mL in DMSO $160 In-stock
5 mg $145 In-stock
10 mg $238 In-stock
50 mg $520 In-stock
100 mg $850 In-stock
200 mg Get quote
500 mg Get quote
Size Price Stock Quantity
10 mM * 1 mL in DMSO €157 In-stock
5 mg €142 In-stock
10 mg €233 In-stock
50 mg €510 In-stock
100 mg €833 In-stock
200 mg Get quote
500 mg Get quote

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Inquiry Information
Product name: SB1317
Cat. No.: HY-15166

SB1317 Data Sheet

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    Purity: 99.83%

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    DataSheet

    Pdf Version Network Version

    MSDS

    Pdf Version

    COA

Related Compound Libraries

Compare The Inhibitor Activity of JAK ( IC50 or Ki Value )

Compound Name Bcl-2 Bcl-B Bcl-w ...
ABT-737 30.3 nM  
ABT-263 ≤1 nM, Ki ≤1 nM, Ki  
Obatoclax 3 uM  
...        
Full Table

Biological Activity of SB1317

SB1317(TG-02) is a novel small molecule potent CDK2/JAK2/FLT3 inhibitor with IC50s of 13/73/56 nM respectively.
IC50 Value: 13/73/56 nM(CDK2/JAK2/FLT3)
Target: CDK2/JAK2/FLT3
TG02 is a novel pyrimidine-based multi-kinase inhibitor that inhibits CDKs 1, 2, 7 and 9 together with JAK2 and FLT3. It dose-dependently inhibits signaling pathways downstream of CDKs, JAK2 and FLT3 in cancer cells with the main targets being CDKs. TG02 is anti-proliferative in a broad range of tumor cell lines, inducing G1 cell cycle arrest and apoptosis. In vivo, 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. TG02 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). TG02 is active in various models of leukemia and provide a rationale for the ongoing clinical evaluation of TG02 in patients with advanced leukemias.

Chemical Information

M.Wt 372.46 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C23H24N4O
CAS No 937270-47-8
Solvent & Solubility

DMSO: ≥ 49 mg/mL

Preparing Stock Solutions

1 mg 5 mg 10 mg
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

Clinical Information of SB1317

Product Name Sponsor Only Condition Start Date End Date Phase Last Change Date
SB1317 Tragara Pharmaceuticals Inc Hematological neoplasm 31-AUG-10 31-JUL-13 Phase 1 14-NOV-13
Tragara Pharmaceuticals Inc Chronic lymphocytic leukemia 30-SEP-12 31-AUG-14 Phase 1 14-NOV-13

References on SB1317

Inhibitor Kit

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  • AMG 925

    AMG 925 is a potent and selective dual inhibtor of CDK4/FLT3 with IC50s of 1.5 nM and 2.4 nM for CDK4 and FLT3, respectively; with IC50 of 19 nM in MOLM-13 cell.

  • Amuvatinib

    Amuvatinib (MP-470) is a potent and multi-targeted inhibitor of c-Kit, PDGFR(alpha) and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively.

  • AST 487

    AST487(NVP-AST487) is a Ret kinase inhibitor/FLT3 inhibitor with IC50 of 0.88 uM for Ret.

  • AT9283

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  • AZD-1480

    AZD1480 is a novel ATP-competitive JAK2 inhibitor with IC50 of 0.26 nM, selectivity against JAK3 and Tyk2, and to a smaller extent against JAK1.

  • AZD-5438

    AZD5438 is a potent inhibitor of CDK1/2/9 with IC50 of 16 nM/6 nM/20 nM. It is less potent to CDK5/6.

  • BIO

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  • BMS-265246

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Compound Name Bcl-2 Bcl-B Bcl-w Bcl-xL Mcl-1 Bfl-1 Other target Note
ABT-737 30.3 nM 78.7 nM 197.8 nM
ABT-263 ≤1 nM, Ki ≤1 nM, Ki ≤0.5 nM, Ki
Obatoclax 3 uM 2.9 uM 5 uM
TW-37 290 nM Ki 1110 nM, Ki 360 nM, Ki
ABT-199 10 nM, Ki >10 uM, Ki >10 uM, Ki No inhibition Bcl-2 selective
AT101 320 nM, Ki 480 nM, Ki 180 nM, Ki
HA14-1 9 uM
Gambogic Acid 1.21 uM 0.66 uM 2.02 uM 1.47 uM 0.79 uM 1.06 uM Caspase
(+)-Apogossypol 0.5-2 uM 0.5-2 uM 0.5-2 uM 0.5-2 uM 0.5-2 uM No inhibition
Mcl1-IN-1 No inhibition 2.4 uM Mcl1 selective
MIM1 >50 uM 4.8 uM Mcl1 selective
Pyridoclax 25 nM, Kd