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THZ1

Item № 9002215
CAS № 1604810-83-4
Purity ≥95%
product image
                (CAS 1604810-83-4)
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL
     500 µg $28.00 0.00
     1 mg $50.00 0.00
     5 mg $112.00 0.00
     10 mg $196.00 0.00

Pricing updated 2019-07-18. Prices are subject to change without notice.

Description

THZ1 is a Cdk7 inhibitor (IC50s = 3.2-15.6 nM in vitro) that selectively targets a remote cysteine residue located outside of the classic kinase domain.1 THZ1 also targets Cdk12 kinase activity although at a higher concentration (IC50 = 250 nM).1 It displays broad anti-proliferative activity against cancer cell lines, particularly T-ALL cell lines that display characteristic misregulation of T cell lineage-specific transcription factors.1 THZ1 is reported to induce apoptotic cell death in triple-negative breast cancer cells that are highly dependent on Cdk7.2

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Technical Information
Formal Name
N-[3-[[5-chloro-4-(1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-4-[[(2E)-4-(dimethylamino)-1-oxo-2-buten-1-yl]amino]-benzamide
CAS Number
1604810-83-4
Molecular Formula
C31H28ClN7O2
Formula Weight
566.1
Purity
≥95%
Formulation
A crystalline solid
λmax
214, 295 nm
SMILES
CN(C/C=C/C(NC1=CC=C(C(NC2=CC(NC3=NC=C(Cl)C(C4=CNC5=C4C=CC=C5)=N3)=CC=C2)=O)C=C1)=O)C
InChI Code
InChI=1S/C31H28ClN7O2/c1-39(2)16-6-11-28(40)35-21-14-12-20(13-15-21)30(41)36-22-7-5-8-23(17-22)37-31-34-19-26(32)29(38-31)25-18-33-27-10-4-3-9-24(25)27/h3-15,17-19,33H,16H2,1-2H3,(H,35,40)(H,36,41)(H,34,37,38)/b11-6+
InChI Key
OBJNFLYHUXWUPF-IZZDOVSWSA-N

Warning - this product is not for human or veterinary use.

Shipping & Storage
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Stability
≥ 2 years
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Additional Information

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References & Product Citations
Product Description References

1. Kwiatkowski, N., Zhang, T., Rahl, P.B., et al. Targeting transcription regulation in cancer with a covalent CDK7 inhibitor Nature 511(7511), 616-620 (2014).

2. Wang, Y., Zhang, T., Kwiatkowski, N., et al. CDK7-dependent transcriptional addiction in triple-negative breast cancer Cell 163(1), 174-186 (2015).

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