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MedKoo Cat#: 526114 | Name: RG-13022
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Description:

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

RG-13022 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 1 µM in HT-22 cells. Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs.

Chemical Structure

RG-13022
RG-13022
CAS#136831-48-6

Theoretical Analysis

MedKoo Cat#: 526114

Name: RG-13022

CAS#: 136831-48-6

Chemical Formula: C16H14N2O2

Exact Mass: 266.1055

Molecular Weight: 266.30

Elemental Analysis: C, 72.17; H, 5.30; N, 10.52; O, 12.02

Price and Availability

Size Price Availability Quantity
100mg USD 750.00 2 Weeks
200mg USD 1,250.00 2 Weeks
500mg USD 2,150.00 2 Weeks
1g USD 2,950.00 2 Weeks
2g USD 4,250.00 2 Weeks
5g USD 6,450.00 2 Weeks
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Related CAS #
No Data
Synonym
RG 13022; RG13022; RG-13022; Tyrphostin RG 13022
IUPAC/Chemical Name
3-Pyridineacetonitrile, alpha-((3,4-dimethoxyphenyl)methylene)-
InChi Key
DBGZNJVTHYFQJI-ZSOIEALJSA-N
InChi Code
InChI=1S/C16H14N2O2/c1-19-15-6-5-12(9-16(15)20-2)8-14(10-17)13-4-3-7-18-11-13/h3-9,11H,1-2H3/b14-8-
SMILES Code
N#C/C(C1=CC=CN=C1)=C/C2=CC=C(OC)C(OC)=C2
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
>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
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
RF9 binds to human NPFF1 and NPFF2 receptors with Ki values of 58 and 75 nM, respectively. It is selective for NPFF1 and NPFF2 receptors over neuropeptide Y (NPY) receptor Y1, GPR10, GPR54, GPR103, ORL-1, and μ-, δ-, and κ-opioid receptors at 10 μM. RF9 (7.5 μM) inhibits NPFF-induced [35S]GTPγS binding to the NPFF2 receptor. It reverses NPVF-induced inhibition of forskolin-stimulated cAMP accumulation in CHO cells expressing the human NPFF1 receptor (EC50 = 4.7 μM). Intracerebroventricular administration of RF9 (10 μg) inhibits NPFF-induced increases in mean arterial pressure and heart rate in rats. It prevents heroin-induced delayed hyperalgesia and associated tolerance in rats when administered subcutaneously at a dose of 0.1 mg/kg.
In vitro activity:
RG-13022 reduced pituitary cell proliferation induced by EGF or E2, showing that the EGF receptor was involved in the induction of mammotroph growth. Reference: Arch Physiol Biochem. 2002 Apr;110(1-2):34-41. https://pubmed.ncbi.nlm.nih.gov/11935398/
In vivo activity:
RG-13022 suppressed squamous cell carcinoma tumor growth in nude mice. RG-13022 also increased the life span of these tumor-bearing nude mice. Reference: Cancer Res. 1991 Aug 15;51(16):4430-5. https://pubmed.ncbi.nlm.nih.gov/1651159/
Solvent mg/mL mM
Solubility
DMSO 100.0 375.52
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 266.30 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. Takahashi S, Sharma S, Oomizu S, Honda J, Takeuchi S. Intrapituitary regulatory system of mammotrophs in the mouse. Arch Physiol Biochem. 2002 Apr;110(1-2):34-41. doi: 10.1076/apab.110.1.34.895. PMID: 11935398. 2. Twaddle GM, Turbov J, Liu N, Murthy S. Tyrosine kinase inhibitors as antiproliferative agents against an estrogen-dependent breast cancer cell line in vitro. J Surg Oncol. 1999 Feb;70(2):83-90. doi: 10.1002/(sici)1096-9098(199902)70:2<83::aid-jso4>3.0.co;2-l. PMID: 10084649. 3. Yoneda T, Lyall RM, Alsina MM, Persons PE, Spada AP, Levitzki A, Zilberstein A, Mundy GR. The antiproliferative effects of tyrosine kinase inhibitors tyrphostins on a human squamous cell carcinoma in vitro and in nude mice. Cancer Res. 1991 Aug 15;51(16):4430-5. PMID: 1651159. 4. Xian W, Kiguchi K, Imamoto A, Rupp T, Zilberstein A, DiGiovanni J. Activation of the epidermal growth factor receptor by skin tumor promoters and in skin tumors from SENCAR mice. Cell Growth Differ. 1995 Nov;6(11):1447-55. PMID: 8562483.
In vitro protocol:
1. Takahashi S, Sharma S, Oomizu S, Honda J, Takeuchi S. Intrapituitary regulatory system of mammotrophs in the mouse. Arch Physiol Biochem. 2002 Apr;110(1-2):34-41. doi: 10.1076/apab.110.1.34.895. PMID: 11935398. 2. Twaddle GM, Turbov J, Liu N, Murthy S. Tyrosine kinase inhibitors as antiproliferative agents against an estrogen-dependent breast cancer cell line in vitro. J Surg Oncol. 1999 Feb;70(2):83-90. doi: 10.1002/(sici)1096-9098(199902)70:2<83::aid-jso4>3.0.co;2-l. PMID: 10084649.
In vivo protocol:
1. Yoneda T, Lyall RM, Alsina MM, Persons PE, Spada AP, Levitzki A, Zilberstein A, Mundy GR. The antiproliferative effects of tyrosine kinase inhibitors tyrphostins on a human squamous cell carcinoma in vitro and in nude mice. Cancer Res. 1991 Aug 15;51(16):4430-5. PMID: 1651159. 2. Xian W, Kiguchi K, Imamoto A, Rupp T, Zilberstein A, DiGiovanni J. Activation of the epidermal growth factor receptor by skin tumor promoters and in skin tumors from SENCAR mice. Cell Growth Differ. 1995 Nov;6(11):1447-55. PMID: 8562483.
1: Komatsu N, Maekawa T, Takeuchi S, Takahashi S. Epidermal growth factor and transforming growth factor-alpha stimulate the proliferation of mouse uterine stromal cells. Zoolog Sci. 2003 May;20(5):639-45. doi: 10.2108/zsj.20.639. PMID: 12777835. 2: Levitzki A. Tyrosine kinases as targets for cancer therapy. Eur J Cancer. 2002 Sep;38 Suppl 5:S11-8. doi: 10.1016/s0959-8049(02)80598-6. PMID: 12528768. 3: Takahashi S, Sharma S, Oomizu S, Honda J, Takeuchi S. Intrapituitary regulatory system of mammotrophs in the mouse. Arch Physiol Biochem. 2002 Apr;110(1-2):34-41. doi: 10.1076/apab.110.1.34.895. PMID: 11935398. 4: Yang H, Wang Z, Miyamoto Y, Reinach PS. Cell signaling pathways mediating epidermal growth factor stimulation of Na:K:2Cl cotransport activity in rabbit corneal epithelial cells. J Membr Biol. 2001 Sep 15;183(2):93-101. doi: 10.1007/s00232-001-0057-6. PMID: 11562791. 5: Oomizu S, Honda J, Takeuchi S, Kakeya T, Masui T, Takahashi S. Transforming growth factor-alpha stimulates proliferation of mammotrophs and corticotrophs in the mouse pituitary. J Endocrinol. 2000 May;165(2):493-501. doi: 10.1677/joe.0.1650493. PMID: 10810313. 6: Reddy KB, Krueger JS, Kondapaka SB, Diglio CA. Mitogen-activated protein kinase (MAPK) regulates the expression of progelatinase B (MMP-9) in breast epithelial cells. Int J Cancer. 1999 Jul 19;82(2):268-73. doi: 10.1002/(sici)1097-0215(19990719)82:2<268::aid-ijc18>3.0.co;2-4. PMID: 10389762. 7: Bian L, Lei Z, Rao CV. Mitogen-activated protein kinase is involved in epidermal-growth-factor-regulated protein phosphorylation in nuclear membranes isolated from JEG-3 human choriocarcinoma cells. Eur J Biochem. 1998 May 1;253(3):545-51. doi: 10.1046/j.1432-1327.1998.2530545.x. PMID: 9654049. 8: McLeod HL, Brunton VG, Eckardt N, Lear MJ, Robins DJ, Workman P, Graham MA. In vivo pharmacology and anti-tumour evaluation of the tyrphostin tyrosine kinase inhibitor RG13022. Br J Cancer. 1996 Dec;74(11):1714-8. doi: 10.1038/bjc.1996.620. PMID: 8956783; PMCID: PMC2077212. 9: McLaughlin M, Brunton V, Morrison V, Rae A, Cooke T, Bartlett J. Growth inhibition of gastric cancer cell lines by the tyrphostin RG13022 and its effects on intracellular signalling. Int J Oncol. 1996 Mar;8(3):589-96. doi: 10.3892/ijo.8.3.589. PMID: 21544401. 10: Kondapaka BS, Reddy KB. Tyrosine kinase inhibitor as a novel signal transduction and antiproliferative agent: prostate cancer. Mol Cell Endocrinol. 1996 Mar 1;117(1):53-8. doi: 10.1016/0303-7207(95)03725-x. PMID: 8734473. 11: Gulli LF, Palmer KC, Chen YQ, Reddy KB. Epidermal growth factor-induced apoptosis in A431 cells can be reversed by reducing the tyrosine kinase activity. Cell Growth Differ. 1996 Feb;7(2):173-8. PMID: 8822200. 12: Oude Weernink PA, Verheul E, Kerkhof E, van Veelen CW, Rijksen G. Inhibitors of protein tyrosine phosphorylation reduce the proliferation of two human glioma cell lines. Neurosurgery. 1996 Jan;38(1):108-13; discussion 113-4. doi: 10.1097/00006123-199601000-00026. PMID: 8747958. 13: Kumar N, Windisch V, Ammon HL. Photoinstability of some tyrphostin drugs: chemical consequences of crystallinity. Pharm Res. 1995 Nov;12(11):1708-15. doi: 10.1023/a:1016213721861. PMID: 8592674. 14: Xian W, Kiguchi K, Imamoto A, Rupp T, Zilberstein A, DiGiovanni J. Activation of the epidermal growth factor receptor by skin tumor promoters and in skin tumors from SENCAR mice. Cell Growth Differ. 1995 Nov;6(11):1447-55. PMID: 8562483. 15: Piontek M, Hengels KJ, Porschen R, Strohmeyer G. Antiproliferative effect of tyrosine kinase inhibitors in epidermal growth factor-stimulated growth of human gastric cancer cells. Anticancer Res. 1993 Nov-Dec;13(6A):2119-23. PMID: 8297123. 16: Reddy KB, Mangold GL, Tandon AK, Yoneda T, Mundy GR, Zilberstein A, Osborne CK. Inhibition of breast cancer cell growth in vitro by a tyrosine kinase inhibitor. Cancer Res. 1992 Jul 1;52(13):3636-41. PMID: 1617636. 17: Yoneda T, Lyall RM, Alsina MM, Persons PE, Spada AP, Levitzki A, Zilberstein A, Mundy GR. The antiproliferative effects of tyrosine kinase inhibitors tyrphostins on a human squamous cell carcinoma in vitro and in nude mice. Cancer Res. 1991 Aug 15;51(16):4430-5. PMID: 1651159.