WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 510235
CAS#: 193746-75-7
Description: SB-242235 is a potent and selective p38 MAP kinase inhibitor that may be an effective therapy for cytokine-mediated diseases such as autoimmune or inflammatory diseases. SB-242235 demonstrates generally favourable pharmacokinetic properties. Systemic plasma clearance was high in rat, but in the non-rodent species SB-242235 demonstrated low to moderate clearance with plasma half-lives > 4h. Oral bioavailability in each preclinical species was high. In rat and monkey, SB-242235 demonstrated non-linear elimination kinetics that manifested as a decrease in clearance with increasing dose and apparent oral bioavailability > 100% at high oral doses.
MedKoo Cat#: 510235
Name: SB-242235
CAS#: 193746-75-7
Chemical Formula: C18H17N5O3
Exact Mass: 351.13314
Molecular Weight: 351.36
Elemental Analysis: C, 61.53; H, 4.88; N, 19.93; O, 13.66
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Synonym: SB242235; SB 242235; SB242235.
IUPAC/Chemical Name: N-(2,3-Dihydro-7,8-dimethoxyimidazo[1,2-c]quinazolin-5-yl)-3-pyridinecarboxamide
SMILES Code: O=C(C1=CC=CN=C1)NC2=NC3=C(C=CC(OC)=C3OC)C4=NCCN24
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
The following data is based on the product molecular weight 351.36 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 |
1: Ward KW, Proksch JW, Gorycki PD, Yu CP, Ho MY, Bush BD, Levy MA, Smith BR. SB-242235, a selective inhibitor of p38 mitogen-activated protein kinase. II: in vitro and in vivo metabolism studies and pharmacokinetic extrapolation to man. Xenobiotica. 2002 Mar;32(3):235-50. PubMed PMID: 11958562.
2: Ward KW, Proksch JW, Salyers KL, Azzarano LM, Morgan JA, Roethke TJ, McSurdy-Freed JE, Levy MA, Smith BR. SB-242235, a selective inhibitor of p38 mitogen-activated protein kinase. I: preclinical pharmacokinetics. Xenobiotica. 2002 Mar;32(3):221-33. PubMed PMID: 11958561.
3: Badger AM, Roshak AK, Cook MN, Newman-Tarr TM, Swift BA, Carlson K, Connor JR, Lee JC, Gowen M, Lark MW, Kumar S. Differential effects of SB 242235, a selective p38 mitogen-activated protein kinase inhibitor, on IL-1 treated bovine and human cartilage/chondrocyte cultures. Osteoarthritis Cartilage. 2000 Nov;8(6):434-43. PubMed PMID: 11069728.
4: Badger AM, Griswold DE, Kapadia R, Blake S, Swift BA, Hoffman SJ, Stroup GB, Webb E, Rieman DJ, Gowen M, Boehm JC, Adams JL, Lee JC. Disease-modifying activity of SB 242235, a selective inhibitor of p38 mitogen-activated protein kinase, in rat adjuvant-induced arthritis. Arthritis Rheum. 2000 Jan;43(1):175-83. PubMed PMID: 10643714.
