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MedKoo Cat#: 574766 | Name: KP372-1
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

KP372-1 is a specific Akt inhibitor. By blocking Akt signaling, KP372-1 has been shown to inhibit proliferation and to induce apoptosis of thyroid cancer cells. In acute myelogenous leukemia cells, KP372-1 is reported to inhibit the kinase activity of Akt, PDK1, and FLT3, decreasing the colony-forming ability of these cells.

Chemical Structure

KP372-1
KP372-1
CAS#1374996-60-7

Theoretical Analysis

MedKoo Cat#: 574766

Name: KP372-1

CAS#: 1374996-60-7

Chemical Formula: C20H8N12O2

Exact Mass: 448.0893

Molecular Weight: 448.37

Elemental Analysis: C, 53.58; H, 1.80; N, 37.49; O, 7.14

Price and Availability

Size Price Availability Quantity
5mg USD 550.00 2 Weeks
10mg USD 950.00 2 Weeks
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Related CAS #
No Data
Synonym
KP372-1
IUPAC/Chemical Name
6H-indeno[1,2-ε]tetrazolo[1,5-b][1,2,4]triazin-6-one, compd. with 10H-indeno[2,1-ε]tetrazolo[1,5-b][1,2,4]triazin-10-one (1:1)
InChi Key
CWFOAASSUQIXOW-UHFFFAOYSA-N
InChi Code
InChI=1S/2C10H4N6O/c17-9-6-4-2-1-3-5(6)7-8(9)11-10-12-14-15-16(10)13-7;17-9-6-4-2-1-3-5(6)7-8(9)13-16-10(11-7)12-14-15-16/h2*1-4H
SMILES Code
O=C1C2=C(C3=NC4=NN=NN4N=C31)C=CC=C2.O=C(C5=NC6=NN=NN6N=C57)C8=C7C=CC=C8
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
KP372-1 is an Akt inhibitor that inhibits proliferation and induces Apoptosis and anoikis.
In vitro activity:
Notably, this study found that KP372-1 is ~ 10- to 20-fold more potent than β-lapachone, another NQO1 substrate, against pancreatic cancer cells. Mechanistically, these data strongly suggest that reactive oxygen species produced by NQO1-dependent redox cycling of KP372-1 cause robust DNA damage, including DNA breaks. Furthermore, this study found that KP372-1-induced DNA damage hyperactivates the central DNA damage sensor protein poly(ADP-ribose) polymerase 1 (PARP1) and activates caspase-3 to initiate cell death. Reference: Sci Rep. 2020 Nov 19;10(1):20210. https://pubmed.ncbi.nlm.nih.gov/33214574/
In vivo activity:
KP372-1 profoundly suppressed the growth of the H1299 xenografts implanted subcutaneously into nude mice versus vehicle (Figures 4D, 4E and S4C). Reference: Cell Metab. 2015 May 5;21(5):777-89. https://pubmed.ncbi.nlm.nih.gov/25955212/
Solvent mg/mL mM
Solubility
DMF 20.0 44.61
DMSO 18.9 42.22
DMSO:PBS (pH 7.2) (1:1) 0.5 1.12
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 448.37 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Viera T, Patidar PL. DNA damage induced by KP372-1 hyperactivates PARP1 and enhances lethality of pancreatic cancer cells with PARP inhibition. Sci Rep. 2020 Nov 19;10(1):20210. doi: 10.1038/s41598-020-76850-4. PMID: 33214574; PMCID: PMC7677541. 2. Mandal M, Younes M, Swan EA, Jasser SA, Doan D, Yigitbasi O, McMurphey A, Ludwick J, El-Naggar AK, Bucana C, Mills GB, Myers JN. The Akt inhibitor KP372-1 inhibits proliferation and induces apoptosis and anoikis in squamous cell carcinoma of the head and neck. Oral Oncol. 2006 Apr;42(4):430-9. doi: 10.1016/j.oraloncology.2005.09.011. Epub 2006 Jan 27. PMID: 16442835; PMCID: PMC1414640. 3. Zhao Y, Hu Q, Cheng F, Su N, Wang A, Zou Y, Hu H, Chen X, Zhou HM, Huang X, Yang K, Zhu Q, Wang X, Yi J, Zhu L, Qian X, Chen L, Tang Y, Loscalzo J, Yang Y. SoNar, a Highly Responsive NAD+/NADH Sensor, Allows High-Throughput Metabolic Screening of Anti-tumor Agents. Cell Metab. 2015 May 5;21(5):777-89. doi: 10.1016/j.cmet.2015.04.009. PMID: 25955212; PMCID: PMC4427571.
In vitro protocol:
1. Viera T, Patidar PL. DNA damage induced by KP372-1 hyperactivates PARP1 and enhances lethality of pancreatic cancer cells with PARP inhibition. Sci Rep. 2020 Nov 19;10(1):20210. doi: 10.1038/s41598-020-76850-4. PMID: 33214574; PMCID: PMC7677541. 2. Mandal M, Younes M, Swan EA, Jasser SA, Doan D, Yigitbasi O, McMurphey A, Ludwick J, El-Naggar AK, Bucana C, Mills GB, Myers JN. The Akt inhibitor KP372-1 inhibits proliferation and induces apoptosis and anoikis in squamous cell carcinoma of the head and neck. Oral Oncol. 2006 Apr;42(4):430-9. doi: 10.1016/j.oraloncology.2005.09.011. Epub 2006 Jan 27. PMID: 16442835; PMCID: PMC1414640.
In vivo protocol:
1. Zhao Y, Hu Q, Cheng F, Su N, Wang A, Zou Y, Hu H, Chen X, Zhou HM, Huang X, Yang K, Zhu Q, Wang X, Yi J, Zhu L, Qian X, Chen L, Tang Y, Loscalzo J, Yang Y. SoNar, a Highly Responsive NAD+/NADH Sensor, Allows High-Throughput Metabolic Screening of Anti-tumor Agents. Cell Metab. 2015 May 5;21(5):777-89. doi: 10.1016/j.cmet.2015.04.009. PMID: 25955212; PMCID: PMC4427571.
1. Zeng, Z., Samudio, I.J., Zhang, W., et al. Simultaneous inhibition of PDK1/AKT and Fms-like tyrosine kinase 3 signaling by a small-molecule KP372-1 induces mitochondrial dysfunction and apoptosis in acute myelogenous leukemia. Cancer Res. 66(7), 3737-3746 (2006). 2. Mandal, M., Kim, S., Younes, M.N., et al. The Akt inhibitor KP372-1 suppresses Akt activity and cell proliferation and induces apoptosis in thyroid cancer cells. Br. J. Cancer 92(10), 1899-1905 (2005).