API-1
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MedKoo CAT#: 406398

CAS#: 36707-00-3

Description: API-1 is a potent Akt inhibitor, which induces GSK3-dependent, β-TrCP- and FBXW7-mediated Mcl-1 degradation, resulting in induction of apoptosis . API-1 rapidly and potently reduced the levels of Mcl-1 primarily in API-1-senstive lung cancer cell lines. Ectopic expression of Mcl-1 protected cells from induction of apoptosis by API-1. API-1 treatment decreased the half-life of Mcl-1, whereas inhibition of the proteasome with MG132 rescued Mcl-1 reduction induced by API-1. API-1 decreased Mcl-1 levels accompanied with a rapid increase in Mcl-1 phosphorylation (S159/T163). Moreover, inhibition of GSK3 inhibited Mcl-1 phosphorylation and reduction induced by API-1 and antagonized the effect of API-1 on induction of apoptosis.


Chemical Structure

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API-1
CAS# 36707-00-3

Theoretical Analysis

MedKoo Cat#: 406398
Name: API-1
CAS#: 36707-00-3
Chemical Formula: C13H15N5O6
Exact Mass: 337.10223
Molecular Weight: 337.29
Elemental Analysis: C, 46.29; H, 4.48; N, 20.76; O, 28.46

Price and Availability

Size Price Availability Quantity
5.0mg USD 295.0 2 Weeks
10.0mg USD 485.0 2 Weeks
25.0mg USD 865.0 2 Weeks
50.0mg USD 1305.0 2 Weeks
100.0mg USD 2015.0 2 Weeks
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Synonym: API1; API-1; API 1; NSC177233.

IUPAC/Chemical Name: 4-amino-8-((2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxamide

InChi Key: SPBWHPXCWJLQRU-FITJORAGSA-N

InChi Code: InChI=1S/C13H15N5O6/c14-10-6-7(20)4(11(15)23)1-18(12(6)17-3-16-10)13-9(22)8(21)5(2-19)24-13/h1,3,5,8-9,13,19,21-22H,2H2,(H2,15,23)(H2,14,16,17)/t5-,8-,9-,13-/m1/s1

SMILES Code: O=C(C1=CN([C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)C3=NC=NC(N)=C3C1=O)N

Appearance: white 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, not in water

Shelf Life: >2 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

Preparing Stock Solutions

The following data is based on the product molecular weight 337.29 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

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1: Ren H, Koo J, Guan B, Yue P, Deng X, Chen M, Khuri FR, Sun SY. The E3 ubiquitin ligases β-TrCP and FBXW7 cooperatively mediates GSK3-dependent Mcl-1 degradation induced by the Akt inhibitor API-1, resulting in apoptosis. Mol Cancer. 2013 Nov 22;12:146. doi: 10.1186/1476-4598-12-146. PubMed PMID: 24261825.

2: Li B, Ren H, Yue P, Chen M, Khuri FR, Sun SY. The novel Akt inhibitor API-1 induces c-FLIP degradation and synergizes with TRAIL to augment apoptosis independent of Akt inhibition. Cancer Prev Res (Phila). 2012 Apr;5(4):612-20. doi: 10.1158/1940-6207.CAPR-11-0548. Epub 2012 Feb 16. PubMed PMID: 22345097; PubMed Central PMCID: PMC3324640.

API-1

5.0mg / USD 295.0


Additional Information