BI-1347

SKU: orb1225656

Description

BI-1347 is a potent, selective inhibitor of CDK8/cyclinC with IC50 of 1 nM; BI-1347 shows tumor growth inhibition in an in vivo xenograft model, BI-1347 is an excellent small molecule tool inhibitor for testing biological hypotheses in vitro and in vivo.

Key Properties

• CAS Number: 2163056-91-3
• MW: 356.429
• Purity: >98% (HPLC)
• Formula: C₂₂H₂₀N₄O
• SMILES: O=C(N(C)C)CN1N=CC(C2=CC=C(C3=CN=CC4=C3C=CC=C4)C=C2)=C1
• Target: CDK
• Solubility: DMSO: 120 mg/mL (336.68 mM), Need ultrasonic and warming （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

• In Vivo:
  BI-1347 (oral gavage; 10 mg/kg; once daily; 30 d) modulates STAT1 S727 phosphorylation and shows anti-tumor activity In vivo. BI-1347 (oral gavage; 10 mg/kg) intermittent schedule and BI-8382 continuous treatment combination treatment increases efficacy compared to each monotherapy in the mammary carcinoma EMT6 model. Animal model: B16-F10-luc2 syngeneic melanoma model. Dosage: 10 mg/kg. Administration: Oral gavage; 10 mg/kg; once daily; 30 d. Result: Reduced phosphorylation of STAT1 S727 for at least 6 h by 60%. Showed minimal effect on body weight at 10 mg/kg. Showed lower tumor burden both on day 23 and 29, compared to the control group.
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• In Vitro:
  BI-1347 (150 nM; 44 h) enhances granzyme B (GZMB+) production in mouse splenic NK cells. BI-1347 (0.1 nM-10 μM; 24 h) treatment increases perforin secretion from NK92MI cells. Western blot analysis. Cell line: Mouse splenic NK cells. Concentration: 150 nM. Incubation time: 44 hours. Result: Increased the proportion of granzyme B-positive NK cells by approximately 4-fold. Western blot analysis. Cell line: Human NK92MI cells. Concentration: 0.1 nM-10 μM Incubation time: 24 hours. Result: Increased perforin levels with an EC50 value of 7.2 nM.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BI1347

Quick Database Links

Gene Symbol

CDK