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P276-00

Cat. No. M2911
P276-00 Structure
Size Price Availability Quantity
5mg USD 220 In stock
50mg USD 860 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

p276-00 is a novel CDK1, CDK4 and CDK9 inhibitor with IC50 of 79 nM, 63 nM and 20 nM, respectively. P276-00 induces apoptosis in multiple myeloma cells by inhibition of Cdk9-T1 and RNA polymerase II-dependent transcription. P276-00 showed a potent cytotoxic effect against MCL cell lines. P276-00 causes multiple myeloma cell death by disrupting the balance between cell survival and apoptosis through inhibition of transcription and downregulation of Mcl-1. P276-00 alone or in combination is a potential therapeutic molecule to improve patients' outcome in mantle cell lymphoma. P276-00 induces G1-G2 arrest, shows antitumor activity on cisplatin-resistant cells and significant in vivo efficacy in tumor models.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 438.3
Formula C21H20ClNO5.HCl
CAS Number 920113-03-7
Purity >99%
Solubility DMSO 70 mg/mL
Storage at -20°C
References

P276-00, a cyclin-dependent kinase inhibitor, modulates cell cycle and induces apoptosis in vitro and in vivo in mantle cell lymphoma cell lines.
Shirsath NP, et al. Mol Cancer. 2012 Oct 18;11:77. PMID: 23075291.

P276-00, a novel cyclin-dependent inhibitor induces G1-G2 arrest, shows antitumor activity on cisplatin-resistant cells and significant in vivo efficacy in tumor models.
Joshi KS, et al. Mol Cancer Ther. 2007 Mar;6(3):926-34. PMID: 17363487.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: P276-00 supplier, CDK, inhibitors

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