WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H130001
CAS#: N/A
Description: GCN2 inhibitor 39 is a cell-potent GCN2 inhibitor with excellent selectivity. In mice, GCN2 inhibitor 39 engages GCN2 at levels ≥80% with an oral dose of 15 mg/kg BID. In the LL2 syngeneic mouse model, GCN2 inhibitor 39 led to significant tumor growth inhibition as a single agent. Furthermore, the use of GCN2 inhibitor 39 led to the enhancement of tumor growth inhibition mediated by anti-VEGFR, which demonstrates the complementarity of these two mechanisms.
Hodoodo Cat#: H130001
Name: GCN2 inhibitor 39
CAS#: N/A
Chemical Formula: C22H23BrN8OS
Exact Mass: 526.09
Molecular Weight: 527.440
Elemental Analysis: C, 50.10; H, 4.40; Br, 15.15; N, 21.25; O, 3.03; S, 6.08
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Synonym: GCN2 inhibitor 39; GCN2 inhibitor-39; GCN2 inhibitor39;
IUPAC/Chemical Name: (1R,3R)-3-((3-Bromo-1-(4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-6-yl)amino)-N,1-dimethylcyclopentane-1-carboxamide
InChi Key: ASGMFNBUXDJWJJ-JLCFBVMHSA-N
InChi Code: InChI=1S/C22H23BrN8OS/c1-12-28-29-19(33-12)13-4-6-15(7-5-13)31-18-16(17(23)30-31)11-25-21(27-18)26-14-8-9-22(2,10-14)20(32)24-3/h4-7,11,14H,8-10H2,1-3H3,(H,24,32)(H,25,26,27)/t14-,22-/m1/s1
SMILES Code: O=C([C@@]1(C)C[C@H](NC2=NC=C3C(N(C4=CC=C(C5=NN=C(C)S5)C=C4)N=C3Br)=N2)CC1)NC
Appearance: To be determined
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: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
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: General control nonderepressible 2 (GCN2) protein kinase is a cellular stress sensor within the tumor microenvironment (TME), whose signaling cascade has been proposed to contribute to immune escape in tumors.
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The following data is based on the product molecular weight 527.44 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.
| 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: | |
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https://pubs.acs.org/doi/10.1021/acs.jmedchem.2c00736
Jackson JJ, Shibuya GM, Ravishankar B, Adusumilli L, Bradford D, Brockstedt DG, Bucher C, Bui M, Cho C, Colas C, Cutler G, Dukes A, Han X, Hu DX, Jacobson S, Kassner PD, Katibah GE, Ko MYM, Kolhatkar U, Leger PR, Ma A, Marshall L, Maung J, Ng AA, Okano A, Pookot D, Poon D, Ramana C, Reilly MK, Robles O, Schwarz JB, Shakhmin AA, Shunatona HP, Sreenivasan R, Tivitmahaisoon P, Xu M, Zaw T, Wustrow DJ, Zibinsky M. Potent GCN2 Inhibitor Capable of Reversing MDSC-Driven T Cell Suppression Demonstrates In Vivo Efficacy as a Single Agent and in Combination with Anti-Angiogenesis Therapy. J Med Chem. 2022 Oct 13;65(19):12895-12924. doi: 10.1021/acs.jmedchem.2c00736. Epub 2022 Sep 20. PMID: 36127295.
