Size | Price | |
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100mg | ||
250mg | ||
500mg |
Targets |
KRAS-SOS1; KRas G12C (IC50 = 140 nM); KRas G12D (IC50 = 109 nM); KRas G12V (IC50 = 154 nM); KRas G12S (IC50 = 155 nM); KRas Q61H (IC50 = 175 nM); K-Ras WT (IC50 = 106 nM)
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ln Vitro |
SAH-SOS1A (0.625-40 μM) reduces cancer cell viability dose-responsively in cancer cells with IC50 values between 5 and 15 μM that carry G12D, G12C, G12V, G12S, G13D, and Q61H mutations. Similar effects are seen in cancer cells that express wild-type KRAS, such as Colo320-HSR cells and HeLa cells[1].
SAH-SOS1A (5-40 μM; 4 hours) inhibits the phosphorylation of MEK1/2, ERK1/2, and AKT in a dose-responsive manner[1]. |
ln Vivo |
SAH-SOS1A (0.2 μL of 10 mM solution; injection; 48 hours; abdomens of D. melanogaster Ras85DV12/ActinGS) treatment significantly lowers ERK1/2's phosphorylation state[1].
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References |
Molecular Formula |
C100H159N27O28
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Molecular Weight |
2187.53
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Exact Mass |
2187.1881424
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CAS # |
1652561-87-9
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Related CAS # |
SAH-SOS1A TFA;2896737-31-6
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Appearance |
solid
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SMILES |
CCC(C)C(C(=O)NC1(CCCC=CCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC(C)C)C(C)O)CC(=O)N)(C)C(=O)NC(CC(C)C)C(=O)NC(CCCCN)C(=O)NC(C(C)O)C(=O)NC(CCC(=O)O)C(=O)NC(CCC(=O)O)C(=O)NCC(=O)NC(CC(=O)N)C(=O)O)C)NC(=O)CNC(=O)C(CC2=CC=CC=C2)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CCCNC(=N)N)NC(=O)C(CCCNC(=N)N)NC(=O)C
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InChi Key |
IVWNCFWBZZQNEM-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C100H159N27O28/c1-12-55(6)78(123-75(134)52-111-82(140)68(47-59-29-19-17-20-30-59)118-88(146)69(48-60-31-21-18-22-32-60)119-84(142)63(35-28-44-109-98(106)107)114-83(141)61(112-58(9)130)34-27-43-108-97(104)105)93(151)127-100(11)41-25-16-14-13-15-24-40-99(10,126-90(148)70(49-72(102)131)120-92(150)80(57(8)129)125-89(147)67(46-54(4)5)122-96(100)155)95(154)121-66(45-53(2)3)87(145)115-62(33-23-26-42-101)86(144)124-79(56(7)128)91(149)117-65(37-39-77(137)138)85(143)116-64(36-38-76(135)136)81(139)110-51-74(133)113-71(94(152)153)50-73(103)132/h13-14,17-22,29-32,53-57,61-71,78-80,128-129H,12,15-16,23-28,33-52,101H2,1-11H3,(H2,102,131)(H2,103,132)(H,110,139)(H,111,140)(H,112,130)(H,113,133)(H,114,141)(H,115,145)(H,116,143)(H,117,149)(H,118,146)(H,119,142)(H,120,150)(H,121,154)(H,122,155)(H,123,134)(H,124,144)(H,125,147)(H,126,148)(H,127,151)(H,135,136)(H,137,138)(H,152,153)(H4,104,105,108)(H4,106,107,109)
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Chemical Name |
4-[[2-[[2-[[2-[[2-[[20-[[2-[[2-[[2-[[2-[[2-[(2-acetamido-5-carbamimidamidopentanoyl)amino]-5-carbamimidamidopentanoyl]amino]-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]acetyl]amino]-3-methylpentanoyl]amino]-8-(2-amino-2-oxoethyl)-5-(1-hydroxyethyl)-11,20-dimethyl-2-(2-methylpropyl)-3,6,9,21-tetraoxo-1,4,7,10-tetrazacyclohenicos-15-ene-11-carbonyl]amino]-4-methylpentanoyl]amino]-6-aminohexanoyl]amino]-3-hydroxybutanoyl]amino]-4-carboxybutanoyl]amino]-5-[[2-[(3-amino-1-carboxy-3-oxopropyl)amino]-2-oxoethyl]amino]-5-oxopentanoic acid
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Synonyms |
SAH-SOS1A
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 0.4571 mL | 2.2857 mL | 4.5714 mL | |
5 mM | 0.0914 mL | 0.4571 mL | 0.9143 mL | |
10 mM | 0.0457 mL | 0.2286 mL | 0.4571 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NMR analysis of SAH-SOS1A/KRAS interaction. Proc Natl Acad Sci U S A . 2015 Feb 10;112(6):1761-6. td> |
SAH-SOS1A inhibits nucleotide association with wild-type and mutant KRAS. Proc Natl Acad Sci U S A . 2015 Feb 10;112(6):1761-6. td> |
SAH-SOS1A cytotoxicity correlates with KRAS binding activity. Proc Natl Acad Sci U S A . 2015 Feb 10;112(6):1761-6. td> |
SAH-SOS1A inhibits phosphosignaling downstream of KRAS in vitro and in vivo. Proc Natl Acad Sci U S A . 2015 Feb 10;112(6):1761-6. td> |