MedKoo Biosciences, Inc.
Tel:   +1-919-636-5577    Fax:   +1-919-980-4831    Email:   sales@medkoo.com
Search
Login Register
Search
MedKoo Cat#: 127554 | Name: ART0380
Featured

Description:

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

ART0380 is a potent and selective ATR inhibitor with a compelling in vitro and in vivo pharmacological profile. ART0380 had potent, selective antitumor activity in a range of preclinical cancer models with differing degrees of ATM LOF. ART0380 was readily absorbed and quickly eliminated upon oral dosing inpreclinical species and was predicted to have a similar PK profilein human. ART0380 was rapidly absorbed and eliminatedwith a mean half-life of ∼8.5 h.21 The PK profile was consistentacross all doses evaluated and characterized by dose-propor-tional exposure with a linear increase in both Cmax and AUC andlow variability observed. ART0380 showed a PK profileconducive to both intermittent and continuous once-daily(QD) dosing.

Chemical Structure

ART0380
ART0380
CAS#2267316-76-5

Theoretical Analysis

MedKoo Cat#: 127554

Name: ART0380

CAS#: 2267316-76-5

Chemical Formula: C18H24N6O2S

Exact Mass: 388.1681

Molecular Weight: 388.49

Elemental Analysis: C, 55.65; H, 6.23; N, 21.63; O, 8.24; S, 8.25

Price and Availability

Size Price Availability Quantity
5mg USD 550.00 2 Weeks
Bulk Inquiry
Buy Now
Add to Cart
Related CAS #
No Data
Synonym
ART0380; ART-0380; ART 0380; alnodesertibum; alnodesertib
IUPAC/Chemical Name
((2-(2-aminopyridin-4-yl)-6-((R)-3-methylmorpholino)pyrimidin-4-yl)imino)(cyclopropyl)(methyl)-l6-sulfanone
InChi Key
JHPDHYAMSPMBIF-ZJGDTTMNSA-N
InChi Code
InChI=1S/C18H24N6O2S/c1-12-11-26-8-7-24(12)17-10-16(23-27(2,25)14-3-4-14)21-18(22-17)13-5-6-20-15(19)9-13/h5-6,9-10,12,14H,3-4,7-8,11H2,1-2H3,(H2,19,20)/t12-,27?/m1/s1
SMILES Code
CC1COCCN1C2=NC(=NC(=C2)N=S(=O)(C)C3CC3)C4=CC(=NC=C4)N
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
Mutations in the ATM gene are common in multiple cancers, but clinical studies of therapies targeting ATM-aberrant cancers have yielded mixed results. Refinement of ATM loss of function (LOF) as a predictive biomarker of response is urgently needed.

Preparing Stock Solutions

The following data is based on the product molecular weight 388.49 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
1: Carroll CL, Johnson MG, Ding Y, Kang Z, Vijayan RSK, Bardenhagen JP, Fang C, Lapointe D, Li M, Liu CY, Lv X, Ma X, Pang J, Shepard HE, Suarez C, Yau AJ, Williams CC, Wu Q, Heald RA, Robinson HMR, Smith GCM, Cross JB, Do MKG, Jiang Y, Lively S, Yap TA, Giuliani V, Heffernan T, Jones P, Di Francesco ME. Discovery of ART0380, a Potent and Selective ATR Kinase Inhibitor Undergoing Phase 2 Clinical Studies for the Treatment of Advanced or Metastatic Solid Cancers. J Med Chem. 2024 Dec 4. doi: 10.1021/acs.jmedchem.4c01595. Epub ahead of print. PMID: 39630604. 2: Ngoi NYL, Gallo D, Torrado C, Nardo M, Durocher D, Yap TA. Synthetic lethal strategies for the development of cancer therapeutics. Nat Rev Clin Oncol. 2024 Dec 3. doi: 10.1038/s41571-024-00966-z. Epub ahead of print. PMID: 39627502. 3: Jacomina LE, Swanson DM, Mitchell MP, Woodward WA, Smith BD, Hoffman KE, Goodman CR, Garber HR, Sun SX, Yap TA, Meric-Bernstam F, Arzu IY, Bloom ES, Schlembach PJ, Strom EA, Stauder MC, Shaitelman SF. Outcomes After Palliative Radiotherapy in Patients with Symptomatic Locoregionally Advanced Breast Cancer. Int J Radiat Oncol Biol Phys. 2024 Nov 14:S0360-3016(24)03637-X. doi: 10.1016/j.ijrobp.2024.11.065. Epub ahead of print. PMID: 39549757. 4: Fontana E, Rosen E, Lee EK, Højgaard M, Mettu NB, Lheureux S, Carneiro BA, Cote GM, Carter L, Plummer R, Mahalingam D, Fretland AJ, Schonhoft JD, Silverman IM, Wainszelbaum M, Xu Y, Ulanet D, Koehler M, Yap TA. Ataxia telangiectasia and Rad3-related (ATR) inhibitor camonsertib dose optimization in patients with biomarker-selected advanced solid tumors (TRESR study). J Natl Cancer Inst. 2024 Sep 1;116(9):1439-1449. doi: 10.1093/jnci/djae098. PMID: 38710487; PMCID: PMC11378309. 5: Nakazawa MS, Silverman IM, Rimkunas V, Veloso A, Glodzik D, Johnson A, Ohsumi TK, Patel SR, Conley AP, Roland CL, Soliman PT, Beird HC, Wu CC, Ingram DR, Lazcano R, Song D, Wani KM, Lazar AJ, Yap TA, Wang WL, Livingston JA. Loss of the DNA Repair Gene RNase H2 Identifies a Unique Subset of DDR-Deficient Leiomyosarcomas. Mol Cancer Ther. 2024 Jul 2;23(7):1057-1065. doi: 10.1158/1535-7163.MCT-23-0761. PMID: 38561019; PMCID: PMC11321279. 6: Pilié PG, Giuliani V, Wang WL, McGrail DJ, Bristow CA, Ngoi NYL, Kyewalabye K, Wani KM, Le H, Campbell E, Sanchez NS, Yang D, Gheeya JS, Goswamy RV, Holla V, Shaw KR, Meric-Bernstam F, Liu CY, Ma X, Feng N, Machado AA, Bardenhagen JP, Vellano CP, Marszalek JR, Rajendra E, Piscitello D, Johnson TI, Likhatcheva M, Elinati E, Majithiya J, Neves J, Grinkevich V, Ranzani M, Luzarraga MR, Boursier M, Armstrong L, Geo L, Lillo G, Tse WY, Lazar AJ, Kopetz SE, Geck Do MK, Lively S, Johnson MG, Robinson HMR, Smith GCM, Carroll CL, Di Francesco ME, Jones P, Heffernan TP, Yap TA. Ataxia-Telangiectasia Mutated Loss-of-Function Displays Variant and Tissue-Specific Differences across Tumor Types. Clin Cancer Res. 2024 May 15;30(10):2121-2139. doi: 10.1158/1078-0432.CCR-23-1763. PMID: 38416404; PMCID: PMC11094420. 7: Pettitt SJ, Shao N, Zatreanu D, Frankum J, Bajrami I, Brough R, Krastev DB, Roumeliotis TI, Choudhary JS, Lorenz S, Rust A, de Bono JS, Yap TA, Tutt ANJ, Lord CJ. A HUWE1 defect causes PARP inhibitor resistance by modulating the BRCA1-∆11q splice variant. Oncogene. 2023 Sep;42(36):2701-2709. doi: 10.1038/s41388-023-02782-8. Epub 2023 Jul 25. PMID: 37491606; PMCID: PMC10473960. 8: Johnson A, Ng PK, Kahle M, Castillo J, Amador B, Wang Y, Zeng J, Holla V, Vu T, Su F, Kim SH, Conway T, Jiang X, Chen K, Shaw KRM, Yap TA, Rodon J, Mills GB, Meric-Bernstam F. Actionability classification of variants of unknown significance correlates with functional effect. NPJ Precis Oncol. 2023 Jul 15;7(1):67. doi: 10.1038/s41698-023-00420-w. PMID: 37454202; PMCID: PMC10349825. 9: Alhalabi O, Groisberg R, Zinner R, Hahn AW, Naing A, Zhang S, Tsimberidou AM, Rodon J, Fu S, Yap TA, Hong DS, Sun M, Jiang Y, Pant S, Shah AY, Zurita A, Tannir NM, Vikram R, Roszik J, Meric-Bernstam F, Subbiah V. Phase I study of sapanisertib with carboplatin and paclitaxel in mTOR pathway altered solid malignancies. NPJ Precis Oncol. 2023 Apr 18;7(1):37. doi: 10.1038/s41698-023-00369-w. PMID: 37072571; PMCID: PMC10113233. 10: Vo HH, Fu S, Hong DS, Karp DD, Piha-Paul S, Subbiah V, Janku F, Naing A, Yap TA, Rodon J, Ajani JA, Cartwright C, Johnson A, Song IW, Beck J, Kahle M, Nogueras-Gonzalez GM, Miller V, Chao C, Vining DJ, Berry DA, Meric-Bernstam F, Tsimberidou AM. Challenges and opportunities associated with the MD Anderson IMPACT2 randomized study in precision oncology. NPJ Precis Oncol. 2022 Oct 27;6(1):78. doi: 10.1038/s41698-022-00317-0. PMID: 36302890; PMCID: PMC9612600.

View History

AEG-41174

AEG-41174

Verubulin

Verubulin

GNE-900

GNE-900

BNC-105p free acid

BNC-105p free acid

cAIMP

cAIMP

LOR17

LOR17